Journal articles on the topic 'Cannabinoids'
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1
Thomas, Fabian Johannes, and Oliver Kayser. "Minor Cannabinoids of Cannabis sativa L." Journal of Medical Science 88, no. 3 (October 1, 2019): 141–49. http://dx.doi.org/10.20883/jms.367.
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Cannabinoids from Cannabis sativa L. play an important role as natural products in clinics. The major cannabinoids compromise tetrahydrocannabinolic acid (THCA) and cannabidiolic acid (CBDA) and its decarboxylated analogs. In this review, we focus on often neglected minor cannabinoids and discuss biosynthetic and chemical degradation routes to other neglected cannabinoids in Cannabis sativa starting from THCA, CBDA and cannabichromenic acid (CBCA). Based on the literature, patents and scientific reports, essential routes for the chemical modification of cannabinoids are discussed to explain chemical diversity chemical conversion and degradation by UV light, as well as temperature and pH leading to the formation of structurally unusual cannabinoids in planta called as minor cannabinoids. Based on known bioorganic reaction schemes and organic chemistry, principles for minor cannabinoid formation like [2+2] cycloaddition, Markonov condensation, radical introduction, or aromatization are discussed. Finally, the non-aqueous environment in Cannabis sativa trichomes is analyzed to clarify their role of a miniaturized bioreactors the light-induced conversion in a non-aqueous enviroment. The overall objective is to bridge from metabolic profiling via cannabinomics to structural and chemical diversity that allows the definition of patterns with consequences also to pharmacology and plant breeding.
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Radwan, Mohamed M., Suman Chandra, Shahbaz Gul, and Mahmoud A. ElSohly. "Cannabinoids, Phenolics, Terpenes and Alkaloids of Cannabis." Molecules 26, no. 9 (May 8, 2021): 2774. http://dx.doi.org/10.3390/molecules26092774.
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Cannabis sativa is one of the oldest medicinal plants in the world. It was introduced into western medicine during the early 19th century. It contains a complex mixture of secondary metabolites, including cannabinoids and non-cannabinoid-type constituents. More than 500 compounds have been reported from C. sativa, of which 125 cannabinoids have been isolated and/or identified as cannabinoids. Cannabinoids are C21 terpeno-phenolic compounds specific to Cannabis. The non-cannabinoid constituents include: non-cannabinoid phenols, flavonoids, terpenes, alkaloids and others. This review discusses the chemistry of the cannabinoids and major non-cannabinoid constituents (terpenes, non-cannabinoid phenolics, and alkaloids) with special emphasis on their chemical structures, methods of isolation, and identification.
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Walker, J. Michael, Nicole M. Strangman, and Susan M. Huang. "Cannabinoids and Pain." Pain Research and Management 6, no. 2 (2001): 74–79. http://dx.doi.org/10.1155/2001/413641.
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Cannabinoids have been used to treat pain for many centuries. However, only during the past several decades have rigorous scientific methods been applied to understand the mechanisms of cannabinoid action. Cannabinoid receptors were discovered in the late 1980s and have been found to mediate the effects of cannabinoids on the nervous system. Several endocannabinoids were subsequently identified. Many studies of cannabinoid analgesia in animals during the past century showed that cannabinoids block all types of pain studied. These effects were found to be due to the suppression of spinal and thalamic nociceptive neurons, independent of any actions on the motor systems. Spinal, supraspinal and peripheral sites of cannabinoid analgesia have been identified. Endocannabinoids are released upon electrical stimulation of the periaqueductal gray, and in response to inflammation in the extremities. These observations and others thus suggest that a natural function of cannabinoid receptors and their endogenous ligands is to regulate pain sensitivity. The therapeutic potential of cannabinoids remains an important topic for future investigations, with previous work suggesting utility in clinical studies of cancer and surgical pain. New modes of delivery and/or new compounds lacking the psychotropic properties of the standard cannabinoid ligands offer promise for cannabinoid therapeutics for pain.
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Voicu, Victor, Felix-Mircea Brehar, Corneliu Toader, Razvan-Adrian Covache-Busuioc, Antonio Daniel Corlatescu, Andrei Bordeianu, Horia Petre Costin, Bogdan-Gabriel Bratu, Luca-Andrei Glavan, and Alexandru Vlad Ciurea. "Cannabinoids in Medicine: A Multifaceted Exploration of Types, Therapeutic Applications, and Emerging Opportunities in Neurodegenerative Diseases and Cancer Therapy." Biomolecules 13, no. 9 (September 14, 2023): 1388. http://dx.doi.org/10.3390/biom13091388.
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In this review article, we embark on a thorough exploration of cannabinoids, compounds that have garnered considerable attention for their potential therapeutic applications. Initially, this article delves into the fundamental background of cannabinoids, emphasizing the role of endogenous cannabinoids in the human body and outlining their significance in studying neurodegenerative diseases and cancer. Building on this foundation, this article categorizes cannabinoids into three main types: phytocannabinoids (plant-derived cannabinoids), endocannabinoids (naturally occurring in the body), and synthetic cannabinoids (laboratory-produced cannabinoids). The intricate mechanisms through which these compounds interact with cannabinoid receptors and signaling pathways are elucidated. A comprehensive overview of cannabinoid pharmacology follows, highlighting their absorption, distribution, metabolism, and excretion, as well as their pharmacokinetic and pharmacodynamic properties. Special emphasis is placed on the role of cannabinoids in neurodegenerative diseases, showcasing their potential benefits in conditions such as Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, and multiple sclerosis. The potential antitumor properties of cannabinoids are also investigated, exploring their potential therapeutic applications in cancer treatment and the mechanisms underlying their anticancer effects. Clinical aspects are thoroughly discussed, from the viability of cannabinoids as therapeutic agents to current clinical trials, safety considerations, and the adverse effects observed. This review culminates in a discussion of promising future research avenues and the broader implications for cannabinoid-based therapies, concluding with a reflection on the immense potential of cannabinoids in modern medicine.
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Huffman, J. W., and J. A. H. Lainton. "Recent Developments Cannabinoids in the Medicinal Chemistry of Cannabinoids." Current Medicinal Chemistry 3, no. 2 (April 1996): 101–16. http://dx.doi.org/10.2174/092986730302220302094839.
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Abstract: As a result of the recognition of a cannabinoid receptor, the isolation of the first endogenous cannabinoid and, more recently, the significant discovery of a cannabinoid antagonist, there has been a resurgence of interest in the medicinal chemistry of cannabinoids. This has included inter alia investigations into the effects of side chain substitution and overall molecular geometry on the biological activity of traditional cannabi noids, which are partially reduced dibenzopyrans, as well as the design and synthesis of a variety of non-traditional cannabinoids. These compounds include indole and pyrrole derivatives, which are agonists, a diarylpyrazole, which is the first cannabinoid antagonist, and various amides of arachidonic acid. The latter compounds are patterned on anandamide (arachidonic acid ethanolamide), the first endogenous cannabinoid isolated from mammalian brain tissue. Modeling studies of the cannabinoid receptor are beginning to provide some insight into the interaction of various agonists with the receptor. This article will review recent developments in the medicinal chemistry of cannabinoids with an emphasis on work reported since 1992.
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Sun, Yan, and Andy Bennett. "Cannabinoids: A New Group of Agonists of PPARs." PPAR Research 2007 (2007): 1–7. http://dx.doi.org/10.1155/2007/23513.
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Cannabinoids have been used medicinally and recreationally for thousands of years and their effects were proposed to occur mainly via activation of the G-protein-coupled receptorCB1/CB2(cannabinoid receptor 1/2). Discovery of potent synthetic analogs of the natural cannabinoids as clinically useful drugs is the sustained aim of cannabinoid research. This demands that these new compounds be free of the psychotropic effects that connected with the recreational use of cannabinoids. In preclinical studies cannabinoids displayed many of the characteristics of nonsteroidal anti-inflammatory drugs (NSAIDs) and it seems to be free of unwanted side effects. An increasing number of therapeutic actions of cannabinoid are being reported that do not appear to be mediated by eitherCB1orCB2, and recently nuclear receptor superfamily PPARs (peroxisome-proliferator-activated receptors) have been suggested as the target of certain cannabinoids. This review summarizes the evidence for cannabinoid activation on PPARs and possible associated remedial potentials.
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Sun, Y., S. P. H. Alexander, D. A. Kendall, and A. J. Bennett. "Cannabinoids and PPARα signalling." Biochemical Society Transactions 34, no. 6 (October 25, 2006): 1095–97. http://dx.doi.org/10.1042/bst0341095.
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Cannabinoids have been shown to possess anti-inflammatory and neuroprotective properties, which were proposed to occur mainly via activation of the G-protein-coupled receptor CB1 (cannabinoid receptor 1). Recently, certain cannabinoids have been reported to be ligands for members of the nuclear receptor transcription factor superfamily known as PPARs (peroxisome-proliferator-activated receptors). This review summarizes the evidence for cannabinoid activation of PPARs and identifies a new intracellular target for cannabinoids as therapeutic agents for neuroprotective treatment.
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Xiong, Wei, Tanxing Cui, Kejun Cheng, Fei Yang, Shao-Rui Chen, Dan Willenbring, Yun Guan, et al. "Cannabinoids suppress inflammatory and neuropathic pain by targeting α3 glycine receptors." Journal of Experimental Medicine 209, no. 6 (May 14, 2012): 1121–34. http://dx.doi.org/10.1084/jem.20120242.
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Certain types of nonpsychoactive cannabinoids can potentiate glycine receptors (GlyRs), an important target for nociceptive regulation at the spinal level. However, little is known about the potential and mechanism of glycinergic cannabinoids for chronic pain treatment. We report that systemic and intrathecal administration of cannabidiol (CBD), a major nonpsychoactive component of marijuana, and its modified derivatives significantly suppress chronic inflammatory and neuropathic pain without causing apparent analgesic tolerance in rodents. The cannabinoids significantly potentiate glycine currents in dorsal horn neurons in rat spinal cord slices. The analgesic potency of 11 structurally similar cannabinoids is positively correlated with cannabinoid potentiation of the α3 GlyRs. In contrast, the cannabinoid analgesia is neither correlated with their binding affinity for CB1 and CB2 receptors nor with their psychoactive side effects. NMR analysis reveals a direct interaction between CBD and S296 in the third transmembrane domain of purified α3 GlyR. The cannabinoid-induced analgesic effect is absent in mice lacking the α3 GlyRs. Our findings suggest that the α3 GlyRs mediate glycinergic cannabinoid-induced suppression of chronic pain. These cannabinoids may represent a novel class of therapeutic agents for the treatment of chronic pain and other diseases involving GlyR dysfunction.
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Irving, Andrew J., Mark G. Rae, and Angela A. Coutts. "Cannabinoids on the Brain." Scientific World JOURNAL 2 (2002): 632–48. http://dx.doi.org/10.1100/tsw.2002.139.
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Cannabis has a long history of consumption both for recreational and medicinal uses. Recently there have been significant advances in our understanding of how cannabis and related compounds (cannabinoids) affect the brain and this review addresses the current state of knowledge of these effects. Cannabinoids act primarily via two types of receptor, CB1and CB2, with CB1receptors mediating most of the central actions of cannabinoids. The presence of a new type of brain cannabinoid receptor is also indicated. Important advances have been made in our understanding of cannabinoid receptor signaling pathways, their modulation of synaptic transmission and plasticity, the cellular targets of cannabinoids in different central nervous system (CNS) regions and, in particular, the role of the endogenous brain cannabinoid (endocannabinoid) system. Cannabinoids have widespread actions in the brain: in the hippocampus they influence learning and memory; in the basal ganglia they modulate locomotor activity and reward pathways; in the hypothalamus they have a role in the control of appetite. Cannabinoids may also be protective against neurodegeneration and brain damage and exhibit anticonvulsant activity. Some of the analgesic effects of cannabinoids also appear to involve sites within the brain. These advances in our understanding of the actions of cannabinoids and the brain endocannabinoid system have led to important new insights into neuronal function which are likely to result in the development of new therapeutic strategies for the treatment of a number of key CNS disorders.
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Sharon, Nitzan, Ludmila Yarmolinsky, Boris Khalfin, Sigal Fleisher-Berkovich, and Shimon Ben-Shabat. "Cannabinoids’ Role in Modulating Central and Peripheral Immunity in Neurodegenerative Diseases." International Journal of Molecular Sciences 25, no. 12 (June 10, 2024): 6402. http://dx.doi.org/10.3390/ijms25126402.
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Cannabinoids (the endocannabinoids, the synthetic cannabinoids, and the phytocannabinoids) are well known for their various pharmacological properties, including neuroprotective and anti-inflammatory features, which are fundamentally important for the treatment of neurodegenerative diseases. The aging of the global population is causing an increase in these diseases that require the development of effective drugs to be even more urgent. Taking into account the unavailability of effective drugs for neurodegenerative diseases, it seems appropriate to consider the role of cannabinoids in the treatment of these diseases. To our knowledge, few reviews are devoted to cannabinoids’ impact on modulating central and peripheral immunity in neurodegenerative diseases. The objective of this review is to provide the best possible information about the cannabinoid receptors and immuno-modulation features, peripheral immune modulation by cannabinoids, cannabinoid-based therapies for the treatment of neurological disorders, and the future development prospects of making cannabinoids versatile tools in the pursuit of effective drugs.
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Ruth, Ashley C., Connie M. Gryniewicz-Ruzicka, Michael L. Trehy, Nicole Kornspan, and Gary Coody. "Consistency of Label Claims of Internet-Purchased Hemp Oil and Cannabis Products as Determined using IMS and LC-MS : A Marketplace Survey." Journal of Regulatory Science 4, no. 3 (July 22, 2016): 1–6. http://dx.doi.org/10.21423/jrs-v04n03p001.
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In this paper we describe the use of ion mobility spectrometry (IMS) and liquid chromatography – high resolution mass spectrometry (LC-HRMS) to screen for the presence of cannabinoids and other potential hazards in a set of products with hemp oil and/or cannabinoid label claims purchased via the internet. Preliminary screening was performed using IMS to examine the products for the presence of cannabinoids, illicit drugs or undeclared pharmaceuticals before analysis by LC-HRMS to quantitatively determine the presence of four of the most common naturally occurring cannabinoids while simultaneously qualitatively screening for the presence of nine of the most common cannabinoids. No other illicit drug or undeclared pharmaceutical was detected in any sample from IMS screening. Eighteen of twenty-three samples tested positive for the presence of at least one cannabinoid by LC-HRMS, with three products containing less than 0.01%(w/w) of a cannabinoid. Four products with explicit CBD label claims were found to not contain any CBD, while three products featured levels of cannabinoids below label claim.https://doi.org/10.21423/jrs-v04n03p001 (DOI assigned 5/31/2019)
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Soraya, hiva, Ruohollah Seddigh, Fatemeh Hadi, and Mohammad Faramarzi. "Chemical cannabis; The New Trend of addiction in Iran." Iranian Journal of Psychiatry and Clinical Psychology 28, no. 1 (April 20, 2022): 10. http://dx.doi.org/10.32598/ijpcp.28.1.4010.1.
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Synthetic cannabinoids (SC) are a heterogeneous group of substances with a high affinity for cannabinoid receptors. Unlike Δ9-tetrahydrocannabinol (THC), synthetic cannabinoids are incredibly potent, highly productive, have more affinity for the Cannabinoid receptor type 1 (CB1), and Cannabinoid receptor type 2 (CB2), and are designed to accelerate the effects of tetrahydrocannabinol. Also, there is experimental evidence that SCs acts on non-cannabinoid receptors, such as the 5-HT2B receptor or dopaminergic receptors. (1, 2).
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Ben-Ami Shor, Dana, Ilan Hochman, Nathan Gluck, Oren Shibolet, and Erez Scapa. "The Cytotoxic Effect of Isolated Cannabinoid Extracts on Polypoid Colorectal Tissue." International Journal of Molecular Sciences 23, no. 19 (September 26, 2022): 11366. http://dx.doi.org/10.3390/ijms231911366.
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Purified cannabinoids have been shown to prevent proliferation and induce apoptosis in colorectal carcinoma cell lines. To assess the cytotoxic effect of cannabinoid extracts and purified cannabinoids on both colorectal polyps and normal colonic cells, as well as their synergistic interaction. Various blends were tested to identify the optimal synergistic effect. Methods: Biopsies from polyps and healthy colonic tissue were obtained from 22 patients undergoing colonic polypectomies. The toxicity of a variety of cannabinoid extracts and purified cannabinoids at different concentrations was evaluated. The synergistic effect of cannabinoids was calculated based on the cells’ survival. Isolated cannabinoids illustrated different toxic effects on the viability of cells derived from colorectal polyps. THC-d8 and THC-d9 were the most toxic and exhibited persistent toxicity in all the polyps tested. CBD was more toxic to polypoid cells in comparison to normal colonic cells at a concentration of 15 µM. The combinations of the cannabinoids CBDV, THCV, CBDVA, CBCA, and CBGA exhibited a synergistic inhibitory effect on the viability of cells derived from colon polyps of patients. Isolated cannabinoid compounds interacted synergistically against colonic polyps, and some also possessed a differential toxic effect on polyp and adjacent colonic tissue, suggesting possible future therapeutic value.
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Nouh, Roua A., Ahmed Kamal, and Anwar Abdelnaser. "Cannabinoids and Multiple Sclerosis: A Critical Analysis of Therapeutic Potentials and Safety Concerns." Pharmaceutics 15, no. 4 (April 5, 2023): 1151. http://dx.doi.org/10.3390/pharmaceutics15041151.
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Multiple sclerosis (MS) is a complicated condition in which the immune system attacks myelinated axons in the central nervous system (CNS), destroying both myelin and axons to varying degrees. Several environmental, genetic, and epigenetic factors influence the risk of developing the disease and how well it responds to treatment. Cannabinoids have recently sparked renewed interest in their therapeutic applications, with growing evidence for their role in symptom control in MS. Cannabinoids exert their roles through the endogenous cannabinoid (ECB) system, with some reports shedding light on the molecular biology of this system and lending credence to some anecdotal medical claims. The double nature of cannabinoids, which cause both positive and negative effects, comes from their actions on the same receptor. Several mechanisms have been adopted to evade this effect. However, there are still numerous limitations to using cannabinoids to treat MS patients. In this review, we will explore and discuss the molecular effect of cannabinoids on the ECB system, the various factors that affect the response to cannabinoids in the body, including the role of gene polymorphism and its relation to dosage, assessing the positive over the adverse effects of cannabinoids in MS, and finally, exploring the possible functional mechanism of cannabinoids in MS and the current and future progress of cannabinoid therapeutics.
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Tran, Jonathan, Aaron C. Elkins, German C. Spangenberg, and Simone J. Rochfort. "High-Throughput Quantitation of Cannabinoids by Liquid Chromatography Triple-Quadrupole Mass Spectrometry." Molecules 27, no. 3 (January 24, 2022): 742. http://dx.doi.org/10.3390/molecules27030742.
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The high-throughput quantitation of cannabinoids is important for the cannabis industry. As medicinal products increase, and research into compounds that have pharmacological benefits increase, and the need to quantitate more than just the main cannabinoids becomes more important. This study aims to provide a rapid, high-throughput method for cannabinoid quantitation using a liquid chromatography triple-quadrupole mass spectrometer (LC-QQQ-MS) with an ultraviolet diode array detector (UV-DAD) for 16 cannabinoids: CBDVA, CBDV, CBDA, CBGA, CBG, CBD, THCV, THCVA, CBN, CBNA, THC, Δ8-THC, CBL, CBC, THCA-A and CBCA. Linearity, limit of detection (LOD), limit of quantitation (LOQ), accuracy, precision, recovery and matrix effect were all evaluated. The validated method was used to determine the cannabinoid concentration of four different Cannabis sativa strains and a low THC strain, all of which have different cannabinoid profiles. All cannabinoids eluted within five minutes with a total analysis time of eight minutes, including column re-equilibration. This was twice as fast as published LC-QQQ-MS methods mentioned in the literature, whilst also covering a wide range of cannabinoid compounds.
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Lynch, ME. "Preclinical Science Regarding Cannabinoids as Analgesics: An Overview." Pain Research and Management 10, suppl a (2005): 7A—14A. http://dx.doi.org/10.1155/2005/169093.
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Modern pharmacology of cannabinoids began in 1964 with the isolation and partial synthesis of delta-9-tetrahydrocannabinol, the main psychoactive agent in herbal cannabis. Since then, potent antinociceptive and antihyperalgesic effects of cannabinoid agonists in animal models of acute and chronic pain; the presence of cannabinoid receptors in pain-processing areas of the brain, spinal cord and periphery; and evidence supporting endogenous modulation of pain systems by cannabinoids has provided support that cannabinoids exhibit significant potential as analgesics. The present article presents an overview of the preclinical science.
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Lu, Yan, and Hope D. Anderson. "Cannabinoid signaling in health and disease." Canadian Journal of Physiology and Pharmacology 95, no. 4 (April 2017): 311–27. http://dx.doi.org/10.1139/cjpp-2016-0346.
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Cannabis sativa has long been used for medicinal purposes. To improve safety and efficacy, compounds from C. sativa were purified or synthesized and named under an umbrella group as cannabinoids. Currently, several cannabinoids may be prescribed in Canada for a variety of indications such as nausea and pain. More recently, an increasing number of reports suggest other salutary effects associated with endogenous cannabinoid signaling including cardioprotection. The therapeutic potential of cannabinoids is therefore extended; however, evidence is limited and mechanisms remain unclear. In addition, the use of cannabinoids clinically has been hindered due to pronounced psychoactive side effects. This review provides an overview on the endocannabinoid system, including known physiological roles, and conditions in which cannabinoid receptor signaling has been implicated.
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Kanabus, Joanna, Marcin Bryła, Marek Roszko, Marta Modrzewska, and Adam Pierzgalski. "Cannabinoids—Characteristics and Potential for Use in Food Production." Molecules 26, no. 21 (November 6, 2021): 6723. http://dx.doi.org/10.3390/molecules26216723.
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Scientific demonstrations of the beneficial effects of non-psychoactive cannabinoids on the human body have increased the interest in foods containing hemp components. This review systematizes the latest discoveries relating to the characteristics of cannabinoids from Cannabis sativa L. var. sativa, it also presents a characterization of the mentioned plant. In this review, we present data on the opportunities and limitations of cannabinoids in food production. This article systematizes the data on the legal aspects, mainly the limits of Δ9-THC in food, the most popular analytical techniques (LC-MS and GC-MS) applied to assay cannabinoids in finished products, and the available data on the stability of cannabinoids during heating, storage, and access to light and oxygen. This may constitute a major challenge to their common use in food processing, as well as the potential formation of undesirable degradation products. Hemp-containing foods have great potential to become commercially popular among functional foods, provided that our understanding of cannabinoid stability in different food matrices and cannabinoid interactions with particular food ingredients are expanded. There remains a need for more data on the effects of technological processes and storage on cannabinoid degradation.
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Skolnick, Phil, and Roger Crystal. "Cannabinoid1 (CB-1) receptor antagonists: a molecular approach to treating acute cannabinoid overdose." Journal of Neural Transmission 127, no. 2 (December 31, 2019): 279–86. http://dx.doi.org/10.1007/s00702-019-02132-7.
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AbstractThe legalization of cannabis for both recreational and medical use in the USA has resulted in a dramatic increase in the number of emergency department visits and hospital admissions for acute cannabinoid overdose (also referred to as cannabis intoxication and cannabis poisoning). Both “edibles” (often sold as brownies, cookies, and candies) containing large amounts of Δ9-tetrahydrocannabinol and synthetic cannabinoids (many possessing higher potencies and efficacies than Δ9-tetrahydrocannabinol) are responsible for a disproportionate number of emergency department visits relative to smoked cannabis. Symptoms of acute cannabinoid overdose range from extreme lethargy, ataxia, and generalized psychomotor impairment to feelings of panic and anxiety, agitation, hallucinations, and psychosis. Treatment of acute cannabinoid overdose is currently supportive and symptom driven. Converging lines of evidence indicating many of the symptoms which can precipitate an emergency department visit are mediated through activation of cannabinoid1 receptors. Here, we review the evidence that cannabinoid1 receptor antagonists, originally developed for indications ranging from obesity to smoking cessation and schizophrenia, provide a molecular approach to treating acute cannabinoid overdose.
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Dobovišek, Luka, Fran Krstanović, Simona Borštnar, and Nataša Debeljak. "Cannabinoids and Hormone Receptor-Positive Breast Cancer Treatment." Cancers 12, no. 3 (February 25, 2020): 525. http://dx.doi.org/10.3390/cancers12030525.
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Breast cancer (BC) is the most common cancer in women worldwide. Approximately 70–80% of BCs express estrogen receptors (ER), which predict the response to endocrine therapy (ET), and are therefore hormone receptor-positive (HR+). Endogenous cannabinoids together with cannabinoid receptor 1 and 2 (CB1, CB2) constitute the basis of the endocannabinoid system. Interactions of cannabinoids with hypothalamic–pituitary–gonadal axis hormones are well documented, and two studies found a positive correlation between peak plasma endogenous cannabinoid anandamide with peak plasma 17β-estradiol, luteinizing hormone and follicle-stimulating hormone levels at ovulation in healthy premenopausal women. Do cannabinoids have an effect on HR+ BC? In this paper we review known and possible interactions between cannabinoids and specific HR+ BC treatments. In preclinical studies, CB1 and CB2 agonists (i.e., anandamide, THC) have been shown to inhibit the proliferation of ER positive BC cell lines. There is less evidence for antitumor cannabinoid action in HR+ BC in animal models and there are no clinical trials exploring the effects of cannabinoids on HR+ BC treatment outcomes. Two studies have shown that tamoxifen and several other selective estrogen receptor modulators (SERM) can act as inverse agonists on CB1 and CB2, an interaction with possible clinical consequences. In addition, cannabinoid action could interact with other commonly used endocrine and targeted therapies used in the treatment of HR+ BC.
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Cretu, Brigitte, Alexandra Zamfir, Sandica Bucurica, Andreea Elena Scheau, Ilinca Savulescu Fiedler, Constantin Caruntu, Ana Caruntu, and Cristian Scheau. "Role of Cannabinoids in Oral Cancer." International Journal of Molecular Sciences 25, no. 2 (January 12, 2024): 969. http://dx.doi.org/10.3390/ijms25020969.
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Cannabinoids have incited scientific interest in different conditions, including malignancy, due to increased exposure to cannabis. Furthermore, cannabinoids are increasingly used to alleviate cancer-related symptoms. This review paper aims to clarify the recent findings on the relationship between cannabinoids and oral cancer, focusing on the molecular mechanisms that could link cannabinoids with oral cancer pathogenesis. In addition, we provide an overview of the current and future perspectives on the management of oral cancer patients using cannabinoid compounds. Epidemiological data on cannabis use and oral cancer development are conflicting. However, in vitro studies assessing the effects of cannabinoids on oral cancer cells have unveiled promising anti-cancer features, including apoptosis and inhibition of cell proliferation. Downregulation of various signaling pathways with anti-cancer effects has been identified in experimental models of oral cancer cells exposed to cannabinoids. Furthermore, in some countries, several synthetic or phytocannabinoids have been approved as medical adjuvants for the management of cancer patients undergoing chemoradiotherapy. Cannabinoids may improve overall well-being by relieving anxiety, depression, pain, and nausea. In conclusion, the link between cannabinoid compounds and oral cancer is complex, and further research is necessary to elucidate the potential risks or their protective impact on oral cancer.
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Richards, John R. "Mechanisms for the Risk of Acute Coronary Syndrome and Arrhythmia Associated With Phytogenic and Synthetic Cannabinoid Use." Journal of Cardiovascular Pharmacology and Therapeutics 25, no. 6 (June 26, 2020): 508–22. http://dx.doi.org/10.1177/1074248420935743.
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Phytogenic cannabinoids from Cannabis sativa and synthetic cannabinoids are commonly used substances for their recreational and medicinal properties. There are increasing reports of cardiotoxicity in close temporal association with cannabinoid use in patients with structurally normal hearts and absence of coronary arterial disease. Associated adverse events include myocardial ischemia, conduction abnormalities, arrhythmias, and sudden death. This review details the effects of phytogenic and synthetic cannabinoids on diverse receptors based on evidence from in vitro, human, and animal studies to establish a molecular basis for these deleterious clinical effects. The synergism between endocannabinoid dysregulation, cannabinoid receptor, and noncannabinoid receptor binding, and impact on cellular ion flux and coronary microvascular circulation is delineated. Pharmacogenetic factors placing certain patients at higher risk for cardiotoxicity are also correlated with the diverse effects of cannabinoids.
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Ghosh, Sharmistha, Ramesh K. Ganju, and Jerome E. Groopman. "Cannabinoids Inhibit the CXCL12-Induced Migration of T Lymphocytes." Blood 104, no. 11 (November 16, 2004): 2667. http://dx.doi.org/10.1182/blood.v104.11.2667.2667.
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Abstract Cannabinoids are both exogenous compounds produced by Cannabis sativa, known for their psychoactive properties, and a family of related endogenous ligands whose functions have been recently characterized. The reported effects of cannabinoids on the immune system include inhibition of T lymphocyte proliferation, altered production of cytokines by T helper cells and decreased antibody formation by B cells. Cannabinoid receptors have been detected in several immune cells, including monocytes, macrophages, basophils and B and T lymphocytes. CB2 (Cannabinoid Receptor 2) appears to be the predominant cannabinoid receptor in the immune system, while the CB1 receptor is found primarily in the brain. We observed high levels of CB2 expression in the Jurkat T lymphocyte cell line, while others have reported expression of the CB2 receptor in CD8+ T lymphocytes. Here, we studied the ability of synthetic and endogenous cannabinoids to modulate a key function of T lymphocytes: chemotactic migration in response to the chemokine CXCL12 (also known as stromal cell-derived factor-1). We observed a 40–50% inhibition of CXCL12-induced chemotaxis in Jurkat T cells with the endogenous cannabinoid anandamide (at 15 μM concentration) and with the synthetic cannabinoids CP55,940 and Win-55,212–2 (each at 10 μM concentration). Inhibition occurred in a dose-dependent manner, indicating that it is a regulated, receptor-mediated process. Further studies showed that the inhibition of migration involved, in part, significant down-regulation of the CXCL12 receptor, CXCR4. We are currently elucidating the signaling cascade whereby endogenous cannabinoids may limit T cell migration in response to CXCL12. Thus, cannabinoids may be novel mediators of immunosuppression when clinically desired.
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Abdallah, Faraj W., Nasir Hussain, Tristan Weaver, and Richard Brull. "Analgesic efficacy of cannabinoids for acute pain management after surgery: a systematic review and meta-analysis." Regional Anesthesia & Pain Medicine 45, no. 7 (May 28, 2020): 509–19. http://dx.doi.org/10.1136/rapm-2020-101340.
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BackgroundEvidence regarding the role of cannabinoids in managing acute postoperative pain is conflicting. The purpose of this systematic review and meta-analysis was to determine the analgesic efficacy of perioperative cannabinoid compounds for acute pain management after surgery.MethodsOriginal research articles evaluating the addition of cannabinoids to standard opioid-based systemic analgesia (Control) in the postoperative period were sought. Our primary outcomes were cumulative oral morphine equivalent consumption and rest pain severity at 24 hours postoperatively. We also assessed analgesic consumption in the postanesthesia care unit (PACU), pain scores in PACU, 6 and 12 hours postoperatively, and opioid-related and cannabinoid-related side effects, patient satisfaction, and quality of recovery as secondary outcomes.ResultsEight randomized controlled trials (924 patients) and four observational studies (4259 patients) were analyzed and included. There were insufficient data to pool for quantification of differences in cumulative oral morphine equivalent consumption and rest pain severity at 24 hours postoperatively with the addition of cannabinoids in comparison to Control. Qualitative synthesis revealed no differences in cumulative oral opioid consumption or pain at rest 24 hours postoperatively with the addition of cannabinoids in comparison to Control. Patients receiving cannabinoids appeared to have an increased weighted mean difference 95% CI of pain at 12 hours by 0.83 cm (0.04 to 1.63) (p=0.04). Patients receiving cannabinoids also appeared to have 3.24 times increased odds of developing hypotension postoperatively (95% CI 1.12 to 9.36) (p=0.03). Qualitative and quantitative synthesis revealed no differences in any other secondary outcomes.ConclusionsOur quantitative and qualitative review of the literature suggests that the analgesic role of perioperative cannabinoid compounds is limited, with no clinically important benefits detected when cannabinoids are added to traditional systemic analgesics compared with traditional systemic analgesics alone. Notably, there appears to be a signal towards increased postoperative pain and hypotension associated with the addition of perioperative cannabinoids to traditional systemic analgesics. These results do not support the routine use of cannabinoids to manage acute postoperative pain at the present time.
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Nehretskii, Serhii. "Forensic and Pharmaceutical, Organizational and Legal Studies of Illegal Circulation, Danger and Drug Addiction from Cannabinoids." SSP Modern Pharmacy and Medicine 2, no. 4 (October 26, 2022): 1–15. http://dx.doi.org/10.53933/sspmpm.v2i4.71.
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A forensic and pharmaceutical, organizational and legal study of illegal circulation, danger and drug addiction from cannabinoids was conducted. Psychoactive substances of cannabinoids were classified as narcotic drugs. Global experience in the circulation of cannabis and psychoactive substances was summarized. Also analyzed scientific works of domestic and foreign authors on the subject of the study. The use of cannabinoids by different categories of the population was analyzed. Forensic and pharmaceutical practice on the illegal circulation of narcotic drugs of plant origin was studied. An assessment of the problems of pharmacotherapy of drug patients with cannabinoid addiction was given. An algorithm for determining the status of cannabinoid addiction has been developed.
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Laiko, I. M., S. V. Mishchenko, and A. I. Kyrychenko. "Variability of cannabinoid contents depending on breeding methods." Plant Breeding and Seed Production, no. 119 (July 12, 2021): 24–33. http://dx.doi.org/10.30835/2413-7510.2021.236989.
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Purpose and objectives. To reveal new possibilities for the expression of cannabis genotypes to obtain starting material with increased contents of non-psychotropic cannabinoids, without tetrahydrocannabinol and stabilized biological traits.
Material and methods. In our study, we took Ukrainian hemp cultivars, the populations of which were distinguished by high stability of cannabinoid contents in comparison with foreign cultivars, as a basis. The study was carried out using breeding, biochemical and statistical methods: physical mutagenesis, inbreeding, individual selection, thin-layer and gas-liquid chromatography to evaluate plants for cannabinoids (HP 6890 Series Hewlett Packard chromatograph using an internal standard).
Results and discussion. It was found that gamma rays at a dose of 200 Gy disrupted the genotypic relationships between cannabinoids, with accumulation of their minimum or maximum amounts. Lowering the irradiation dose to 150 Gy does not destabilize the population in terms of the cannabinoid contents.
Inbreeding can be also used in breeding for both to create inbred lines that are homozygous for the ‘no cannabinoids’ trait and to identify lines with increased contents of cannabidiol, cannabigerol or cannabichromen.
A lot of early-bred and modern cultivars (French, Polish, Hungarian, German) show a high population variability of the cannabinoid contents, proving that no systemic breeding was conducted to stabilize these traits in the populations of these cultivars. High homogeneity of populations in terms of the formation and accumulation of cannabinoids is only intrinsic to monoecious hemp cultivars bred by the Institute of Bast Crops of NAAS.
The homozygosity of a population primarily depends on the control of targeted cross-pollination between cannabinoid-free plants using an express testing plants for these compounds prior to anthesis onset and subsequent analysis of the selected elite plants by thin-layer chromatography.
Given the relevance of creating hemp varieties with therapeutic properties, breeding methods have been developed to shift the balance of ‘no cannabinoid at all’ towards a genetically determined increase in one of the cannabinoids (cannabidiol, cannabigerol, cannabichromene) combined with eliminated psychotropic activity (the THC content does not exceed 0.08%).
Studies of cannabinoid accumulation revealed differences in their formation during the growing period. Based on the fact that the maximum accumulation of cannabinoids occurs during the seed ripening onset, and, in particular, their synthesis is the most intensive in perianths and small leaves, it is possible to evaluate the prospects for creating hemp cultivars with a branched diamond-shaped inflorescence, which will provide, in addition to a high content of one or another cannabinoid, an increased yield of plant biomass.
Conclusions. Physical mutagenesis, inbreeding and selection are promising breeding methods for reducing psychotropic tetrahydrocannabinol, stabilizing cannabis cultivars in terms of the absence of cannabinoids, increasing the contents of cannabidiol, cannabigerol and cannabichromene gaining advantage from valuable collection accessions
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Hunziker, Sandra, Federico Morosoli, Kathrin Zuercher, Anne Tscherter, and Sebastian Grunt. "Prescription Practices of Cannabinoids in Children with Cerebral Palsy Worldwide—A Survey of the Swiss Cerebral Palsy Registry." Children 10, no. 12 (November 23, 2023): 1838. http://dx.doi.org/10.3390/children10121838.
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Cannabinoids are prescribed to children with cerebral palsy despite limited evidence. We aimed to assess cannabinoid prescribing practices in children with cerebral palsy, focusing on indications, types of preparations used, and tolerability. Furthermore, we investigated how physicians acquire knowledge about cannabinoid medication. We asked physicians with expertise in the care of children with cerebral palsy about their prescribing practices for cannabinoids. Data were collected through an online survey, which was distributed by email. In addition to the demographic information of participants, we also inquired about the indications for the prescription of cannabinoids, experiences regarding efficacy, and observed side effects of the therapy. Seventy physicians from Europe, North America, and Australia completed the survey. Forty-seven participants were experienced in treating of children with cerebral palsy with cannabinoids. The most common indication was epilepsy (69%), followed by spasticity (64%) and pain (63%). The preparations and doses prescribed varied considerably. Half of the participants evaluated the effect of the cannabinoids as moderate. Twenty-nine physicians reported side effects, most frequently, drowsiness (26%), somnolence (19%), fatigue (13%), and diarrhea (13%). Despite the lack of evidence to date, cannabinoids are used to treat children with cerebral palsy in a wide variety of indications. Randomized controlled trials in this vulnerable patient group are therefore of utmost importance.
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Bow, Eric W., and John M. Rimoldi. "The Structure–Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation." Perspectives in Medicinal Chemistry 8 (January 2016): PMC.S32171. http://dx.doi.org/10.4137/pmc.s32171.
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The cannabinoids are members of a deceptively simple class of terpenophenolic secondary metabolites isolated from Cannabis sativa highlighted by (-)-Δ 9 -tetrahydrocannabinol (THC), eliciting distinct pharmacological effects mediated largely by cannabinoid receptor (CB1 or CB2) signaling. Since the initial discovery of THC and related cannabinoids, synthetic and semisynthetic classical cannabinoid analogs have been evaluated to help define receptor binding modes and structure–CB1/CB2 functional activity relationships. This perspective will examine the classical cannabinoids, with particular emphasis on the structure–activity relationship of five regions: C3 side chain, phenolic hydroxyl, aromatic A-ring, pyran B-ring, and cyclohexenyl C-ring. Cumulative structure–activity relationship studies to date have helped define the critical structural elements required for potency and selectivity toward CB1 and CB2 and, more importantly, ushered the discovery and development of contemporary nonclassical cannabinoid modulators with enhanced physicochemical and pharmacological profiles.
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Sañudo-Peña, M. Clara, and J. Michael Walker. "Role of the Subthalamic Nucleus in Cannabinoid Actions in the Substantia Nigra of the Rat." Journal of Neurophysiology 77, no. 3 (March 1, 1997): 1635–38. http://dx.doi.org/10.1152/jn.1997.77.3.1635.
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Sañudo-Peña, M. Clara and J. Michael Walker. Role of the subthalamic nucleus in cannabinoid actions in the substantia nigra of the rat. J. Neurophysiol. 77: 1635–1638, 1997. The effect of cannabinoids on the excitatory input to the substantia nigra reticulata (SNr) from the subthalamic nucleus was explored. For this purpose a knife cut was performed rostral to the subthalamic nucleus to isolate the subthalamic nucleus and the SNr from the striatum, a major source of cannabinoid receptors to the SNr. The data showed that the cannabinoid agonist WIN55,212-2 blocked the increase in the firing rate of SNr neurons induced by stimulation of the subthalamic nucleus with bicuculline. Furthermore, the cannabinoid antagonist SR141716A antagonized the effect of the cannabinoid agonist. This study showed that cannabinoids regulate not only the striatonigral pathway, as previously reported, but also the subthalamonigral pathway. The opposite influences of these two inputs to the SNr, inhibitory and excitatory respectively, suggest that endogenous cannabinoids play a major role in the physiological regulation of the SNr.
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Ahmed, Ishtiaq, Saif Ur Rehman, Shiva Shahmohamadnejad, Muhammad Anjum Zia, Muhammad Ahmad, Muhammad Muzammal Saeed, Zain Akram, Hafiz M. N. Iqbal, and Qingyou Liu. "Therapeutic Attributes of Endocannabinoid System against Neuro-Inflammatory Autoimmune Disorders." Molecules 26, no. 11 (June 3, 2021): 3389. http://dx.doi.org/10.3390/molecules26113389.
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In humans, various sites like cannabinoid receptors (CBR) having a binding affinity with cannabinoids are distributed on the surface of different cell types, where endocannabinoids (ECs) and derivatives of fatty acid can bind. The binding of these substance(s) triggers the activation of specific receptors required for various physiological functions, including pain sensation, memory, and appetite. The ECs and CBR perform multiple functions via the cannabinoid receptor 1 (CB1); cannabinoid receptor 2 (CB2), having a key effect in restraining neurotransmitters and the arrangement of cytokines. The role of cannabinoids in the immune system is illustrated because of their immunosuppressive characteristics. These characteristics include inhibition of leucocyte proliferation, T cells apoptosis, and induction of macrophages along with reduced pro-inflammatory cytokines secretion. The review seeks to discuss the functional relationship between the endocannabinoid system (ECS) and anti-tumor characteristics of cannabinoids in various cancers. The therapeutic potential of cannabinoids for cancer—both in vivo and in vitro clinical trials—has also been highlighted and reported to be effective in mice models in arthritis for the inflammation reduction, neuropathic pain, positive effect in multiple sclerosis and type-1 diabetes mellitus, and found beneficial for treating in various cancers. In human models, such studies are limited; thereby, further research is indispensable in this field to get a conclusive outcome. Therefore, in autoimmune disorders, therapeutic cannabinoids can serve as promising immunosuppressive and anti-fibrotic agents.
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Costa, Alana C., Helena P. G. Joaquim, João F. C. Pedrazzi, Andreia de O. Pain, Gustavo Duque, and Ivan Aprahamian. "Cannabinoids in Late Life Parkinson’s Disease and Dementia: Biological Pathways and Clinical Challenges." Brain Sciences 12, no. 12 (November 22, 2022): 1596. http://dx.doi.org/10.3390/brainsci12121596.
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The use of cannabinoids as therapeutic drugs has increased among aging populations recently. Age-related changes in the endogenous cannabinoid system could influence the effects of therapies that target the cannabinoid system. At the preclinical level, cannabidiol (CBD) induces anti-amyloidogenic, antioxidative, anti-apoptotic, anti-inflammatory, and neuroprotective effects. These findings suggest a potential therapeutic role of cannabinoids to neurodegenerative disorders such as Parkinson’s disease (PD) and Alzheimer. Emerging evidence suggests that CBD and tetrahydrocannabinol have neuroprotective therapeutic-like effects on dementias. In clinical practice, cannabinoids are being used off-label to relieve symptoms of PD and AD. In fact, patients are using cannabis compounds for the treatment of tremor, non-motor symptoms, anxiety, and sleep assistance in PD, and managing responsive behaviors of dementia such as agitation. However, strong evidence from clinical trials is scarce for most indications. Some clinicians consider cannabinoids an alternative for older adults bearing Parkinson’s disease and Alzheimer’s dementia with a poor response to first-line treatments. In our concept and experience, cannabinoids should never be considered a first-line treatment but could be regarded as an adjuvant therapy in specific situations commonly seen in clinical practice. To mitigate the risk of adverse events, the traditional dogma of geriatric medicine, starting with a low dose and proceeding with a slow titration regime, should also be employed with cannabinoids. In this review, we aimed to address preclinical evidence of cannabinoids in neurodegenerative disorders such as PD and AD and discuss potential off-label use of cannabinoids in clinical practice of these disorders.
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Dorris, Kathleen, Jessica Channell, Ashley Mettetal, Molly Hemenway, Natalie Briones, Alexander Tran, Andrea Griesinger, et al. "QOL-36. USE OF CANNABINOIDS IN THE PEDIATRIC CENTRAL NERVOUS SYSTEM TUMOR POPULATION." Neuro-Oncology 22, Supplement_3 (December 1, 2020): iii438. http://dx.doi.org/10.1093/neuonc/noaa222.695.
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Abstract BACKGROUND Cannabinoids, including cannabidiol (CBD) and tetrahydrocannabinol (THC), are a class of compounds found in marijuana. Numerous studies in adults have examined cannabinoid use in management of cancer-related symptoms such as nausea, anorexia, and pain. Less is known about the use in the pediatric oncology population. METHODS A prospective observational study has been ongoing since 2016 at Children’s Hospital Colorado to evaluate cannabinoids’ impact using PedsQL™ modules on quality of life of pediatric patients with central nervous system (CNS) tumors who are 2–18 years old. Laboratory assessments of T-cell activity and pharmacokinetics of CBD, THC and associated metabolites are in process. Diaries with exploratory information on cannabinoid use patterns are being collected. RESULTS Thirty-three patients (14:19; male:female) have been enrolled with a median age of 6.4 years (range, 2.9–17.7 years). The most common tumor type in enrolled patients is embryonal tumors (13/33; 39%). Nine (27%) patients have low-grade glial/glioneuronal tumors, and eight (24%) had high-grade/diffuse midline gliomas. The remaining patients had ependymoma or craniopharyngioma. The median time on cannabinoids is 9 months. Most (n=20) patients have used oral products with CBD and THC. One patient continues on cannabinoid therapy in follow up. Preliminary immune function analyses identified impaired neutrophil superoxide anion production and chemotaxis in patients taking cannabinoids at early time points on therapy. CONCLUSIONS Families of children with various CNS tumors are pursuing cannabinoid therapy for both antitumor and supportive care purposes. Analysis of the impact of cannabinoids on patients’ quality of life is ongoing.
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Val, Bellman,, Kiolbasa, Megan, Vasquez Franjul, Manuel, Namdev, Vaishalee, Choi, Sarang, and Isola, Sasank. "Medical Cannabis in Palliative Psychiatry: Clinical Aspects of Affective Regulation and Legal Challenges." International Journal of Innovative Research in Medical Science 6, no. 09 (September 16, 2021): 588–607. http://dx.doi.org/10.23958/ijirms/vol06-i09/1203.
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Millions of Americans use cannabis for medical purposes including but not limited to pain, nausea, mood changes and appetite stimulation. The use of cannabinoid in the palliative care setting is a relatively new trend. Given the fact that a patient receiving palliative care is not necessarily approaching death, the increasing need for palliative care as the American population ages, this literature review was compiled in order to examine the potential efficacy of cannabis in treating the mental health comorbidities of palliative care patients. We attempted to create the most comprehensive report on cannabinoid use in palliative psychiatry. It summarizes the most recently published science on cannabinoid use in palliative care patients and its impact on mood and anxiety symptoms. The mechanism of action of cannabinoids on their associated receptors was elucidated, as were the pharmacological roles that specific molecules in cannabinoids, like cannabidiolic acid and terpenes, play in cannabinoids’ overall efficacy. The legal impediments to widespread cannabis use were also explored. While the potential efficacy of cannabinoids has proven to be mixed, more research is necessary to ensure that a potentially vital resource in treating palliative care patients does not go underutilized.
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Almogi-Hazan, Osnat, and Reuven Or. "Cannabis, the Endocannabinoid System and Immunity—the Journey from the Bedside to the Bench and Back." International Journal of Molecular Sciences 21, no. 12 (June 23, 2020): 4448. http://dx.doi.org/10.3390/ijms21124448.
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The Cannabis plant contains numerous components, including cannabinoids and other active molecules. The phyto-cannabinoid activity is mediated by the endocannabinoid system. Cannabinoids affect the nervous system and play significant roles in the regulation of the immune system. While Cannabis is not yet registered as a drug, the potential of cannabinoid-based medicines for the treatment of various conditions has led many countries to authorize their clinical use. However, the data from basic and medical research dedicated to medical Cannabis is currently limited. A variety of pathological conditions involve dysregulation of the immune system. For example, in cancer, immune surveillance and cancer immuno-editing result in immune tolerance. On the other hand, in autoimmune diseases increased immune activity causes tissue damage. Immuno-modulating therapies can regulate the immune system and therefore the immune-regulatory properties of cannabinoids, suggest their use in the therapy of immune related disorders. In this contemporary review, we discuss the roles of the endocannabinoid system in immunity and explore the emerging data about the effects of cannabinoids on the immune response in different pathologies. In addition, we discuss the complexities of using cannabinoid-based treatments in each of these conditions.
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Olivas-Aguirre, Miguel, Cecilia Gutiérrez-Iñiguez, Igor Pottosin, and Oxana Dobrovinskaya. "Molecular Targets for Cannabinoids in Natural Killer Cells: Do They Modulate the Antitumor Activity?" Receptors 3, no. 2 (March 25, 2024): 122–44. http://dx.doi.org/10.3390/receptors3020007.
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Recent research has emphasized the potential of natural and synthetic cannabinoids as anticancer agents. Yet it remains unclear whether and in which sense cannabinoids affect the anticancer activity of NK cells, an important branch of anticancer immunity. Similar uncertainty exists regarding NK cells-based immunotherapy. Here we presented an overview of multiple cannabinoid targets as canonical (mainly CB2) and non-canonical receptors, ion channels, transporters, and enzymes, expressed in NK cells, along with underlying molecular mechanisms. Through them, cannabinoids can affect viability, proliferation, migration, cytokine production, and the overall anticancer activity of NK cells. Respective holistic studies are limited, and, mostly, are phenomenological, not linking observed effects with certain molecular targets. Another problem of existing studies is the lack of standardisation, so that diverse cannabinoids at variable concentrations and ways of administration are applied, and often, instead of purified NK cells, the whole lymphocyte population is used. Therefore, there is an urgent need for more focused, systemic, and in-depth studies of the impact of the cannabinoid toolkit on NK cell function, to critically address the compatibility and potential synergies between NK activity and cannabinoid utilization in the realm of anticancer interventions.
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Barbado, María Victoria, Mayte Medrano, Jose Ignacio Piruat, Ivan Valle, Teresa Caballero, Isabel Álvarez, and Jose Antonio Perez-Simón. "Cannabinoids As Antimyeloma Agents: a New Approach for the Treatment of Multiple Myeloma." Blood 124, no. 21 (December 6, 2014): 4724. http://dx.doi.org/10.1182/blood.v124.21.4724.4724.
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Abstract INTRODUCTION: Cannabinoids are the active components of Cannabis sativa. The interest in cannabinoid research has triggered only two decades ago following the discovery of the endocannabinoid system, mainly from the molecular characterization of endogenous receptors: CB1 (mostly expressed in the central nervous system) and CB2 (in immune cells). In the last few years, several groups have described their use as potential therapeutic agents in the treatment of pain, multiple sclerosis or Alzheimer. Moreover, increasing evidences have suggested their potential role as antitumor drugs. Despite the abundant expression of CB2 in immune cells, very few studies have examined its use in hematological malignancies. Considering the high expression levels of CB2 in B-cells, we hypothesized that plasma cells (PCs) could also express high levels of CB2 and therefore might be an excellent target for cannabinoids. DEVELOPMENT: Our objective was to evaluate the anti-tumor effect of cannabinoids in MM and identify the mechanisms involved. We use the synthetic cannabinoids WIN-55 (CB1 and CB2 mixed agonist) and JWH-133 (CB2 selective agonist). We used MM cell lines U266, MM1R, MM1S and RPMI8226 and primary PCs from patients and CD34+ cells from patients and healthy donors. Viability studies were carried out by MTT and cytometric analyses and the expression of receptors and the study of signaling pathways by Western blot (WB). Further, we tested the cannabinoid effects in vivo in murine models (NSG xenograft mice). We observed a high expression of CBs in CPs and a remarkable proapoptotic effect of cannabinoids on myelomatous cells. By contrast, the viability of the CD34 + hematopoietic progenitor cells remained unaffected irrespective of the dose used. In this regard, in MM cells lines and primary cells from patients we observed cleavage of PARP as well as activation of caspases 8, 9, 3 and 2, the latter related to endoplasmic reticulum stress induced by the cannabinoids. This cannabinoid-induced apoptotic effect was also mediated by AKT and MAPKs signaling pathways, as assessed by WB. In addition, Fluorometric analyses confirmed that cannabinoids induce an early mitochondrial damage. Next we confirmed that cannabinoids increase the expression of SPT, the limiting enzyme for the synthesis of ceramides (membrane sphingolipids). The upregulation of SPT following cannabinoid incubation induced accumulation of ceramide, as assessed by immunohistochemistry. Furthermore, the incubation with myoricine, an SPT inhibitor, partially inhibited caspase 3 activation. Finally, we checked the antimyeloma effect of the cannabinoids in vivo, using a model of human MM xenografted in immunodeficient mice NOD/SCID. Our results demonstrate a significant reduction in tumor growth, even tumor regression, as well as a significant increase of survival of cannabinoid-treated as compared to mice receiving vehicle. CONCLUSIONS: Cannabinoids have a very selective antitumor effect against MM cells. This effect involves activation of apoptosis processes and alterations in the composition of membrane sphingolipids (ceramides). In vivo studies confirmed the efficacy of these agents in the treatment of MM. This study lays the groundwork for the design of new anti-myeloma therapies. Disclosures No relevant conflicts of interest to declare.
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Holst, Pernille, Annemarie Thuri Kristensen, and Maja Louise Arendt. "Danish dog owners’ use and the perceived effect of unlicensed cannabis products in dogs." PLOS ONE 19, no. 1 (January 31, 2024): e0296698. http://dx.doi.org/10.1371/journal.pone.0296698.
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The interest in the use of medical cannabis has increased in recent years in both human and veterinary fields. In Denmark, there are no veterinary-licensed medical cannabis or cannabinoid supplements, and it is illegal to prescribe or sell cannabinoids intended for the treatment of veterinary patients. This study aimed to explore the unlicensed cannabinoid use in Danish dogs, by questioning dog owners about usage, indication for use, way of purchase, and their perceived effect of the cannabinoid treatment. An anonymous online survey was distributed via social media. The total number of respondents were 2,002, of which 38% indicated using or having administered cannabinoids to their dog. The majority of the respondents confirming the use of cannabinoids (93%) had used cannabidiol drops/oil and only few (4%) reported using Δ9-tetrahydrocannabinol-based products. Most owners (67%) purchased the products online. The three most common indications for use were pain alleviation, behavioural issues, and allergy. When asked about the respondent-perceived effect the majority reported a good or very good effect. The indication with the highest percentage of owner-perceived positive effect (77%) was pain alleviation. This study shows that, despite no licensed veterinary cannabinoid products being available in Denmark, dog owners do supplement their dogs with cannabinoids and the majority of these perceive that the treatment had a positive effect. This supports the need for more evidence-based knowledge in veterinary cannabinoid therapy.
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Sommano, Sarana Rose, Piyachat Sunanta, Noppol Leksawasdi, Kittisak Jantanasakulwong, Pornchai Rachtanapun, Phisit Seesuriyachan, Yuthana Phimolsiripol, et al. "Mass Spectrometry-Based Metabolomics of Phytocannabinoids from Non-Cannabis Plant Origins." Molecules 27, no. 10 (May 20, 2022): 3301. http://dx.doi.org/10.3390/molecules27103301.
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Phytocannabinoids are isoprenylated resorcinyl polyketides produced mostly in glandular trichomes of Cannabis sativa L. These discoveries led to the identification of cannabinoid receptors, which modulate psychotropic and pharmacological reactions and are found primarily in the human central nervous system. As a result of the biogenetic process, aliphatic ketide phytocannabinoids are exclusively found in the cannabis species and have a limited natural distribution, whereas phenethyl-type phytocannabinoids are present in higher plants, liverworts, and fungi. The development of cannabinomics has uncovered evidence of new sources containing various phytocannabinoid derivatives. Phytocannabinoids have been isolated as artifacts from their carboxylated forms (pre-cannabinoids or acidic cannabinoids) from plant sources. In this review, the overview of the phytocannabinoid biosynthesis is presented. Different non-cannabis plant sources are described either from those belonging to the angiosperm species and bryophytes, together with their metabolomic structures. Lastly, we discuss the legal framework for the ingestion of these biological materials which currently receive the attention as a legal high.
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GÓMEZ DEL PULGAR, Teresa, Guillermo VELASCO, and Manuel GUZMÁN. "The CB1 cannabinoid receptor is coupled to the activation of protein kinase B/Akt." Biochemical Journal 347, no. 2 (April 10, 2000): 369–73. http://dx.doi.org/10.1042/bj3470369.
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Cannabinoids exert most of their effects in the central nervous system through the CB1 cannabinoid receptor. This G-protein-coupled receptor has been shown to be functionally coupled to inhibition of adenylate cyclase, modulation of ion channels and activation of extracellular-signal-regulated kinase. Using Chinese hamster ovary cells stably transfected with the CB1 receptor cDNA we show here that ∆9-tetrahydrocannabinol (THC), the major active component of marijuana, induces the activation of protein kinase B/Akt (PKB). This effect of THC was also exerted by the endogenous cannabinoid anandamide and the synthetic cannabinoids CP-55940 and HU-210, and was prevented by the selective CB1 antagonist SR141716. Pertussis toxin and wortmannin blocked the CB1 receptor-evoked activation of PKB, pointing to the sequential involvement of a Gi/Go protein and phosphoinositide 3ʹ-kinase. The functionality of the cannabinoid-induced stimulation of PKB was proved by the increased phosphorylation of glycogen synthase kinase-3 serine 21 observed in cannabinoid-treated cells and its prevention by SR141716 and wortmannin. Cannabinoids activated PKB in the human astrocytoma cell line U373 MG, which expresses the CB1 receptor, but not in the human promyelocytic cell line HL-60, which expresses the CB2 receptor. Data indicate that activation of PKB may be responsible for some of the effects of cannabinoids in cells expressing the CB1 receptor.
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Mulvihill, Colleen J., Joshua D. Lutgens, Jimmy D. Gollihar, Petra Bachanová, Caitlin Tramont, Edward M. Marcotte, Andrew D. Ellington, and Elizabeth C. Gardner. "A Humanized CB1R Yeast Biosensor Enables Facile Screening of Cannabinoid Compounds." International Journal of Molecular Sciences 25, no. 11 (May 31, 2024): 6060. http://dx.doi.org/10.3390/ijms25116060.
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Yeast expression of human G-protein-coupled receptors (GPCRs) can be used as a biosensor platform for the detection of pharmaceuticals. Cannabinoid receptor type 1 (CB1R) is of particular interest, given the cornucopia of natural and synthetic cannabinoids being explored as therapeutics. We show for the first time that engineering the N-terminus of CB1R allows for efficient signal transduction in yeast, and that engineering the sterol composition of the yeast membrane modulates its performance. Using an engineered cannabinoid biosensor, we demonstrate that large libraries of synthetic cannabinoids and terpenes can be quickly screened to elucidate known and novel structure–activity relationships. The biosensor strains offer a ready platform for evaluating the activity of new synthetic cannabinoids, monitoring drugs of abuse, and developing therapeutic molecules.
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Polyakova, A. S., and D. B. Rakhmetov. "Change in the content of cannabinoid substances in Cannabis sativa L. inzucht-generations in the plus and minus selections." Faktori eksperimental'noi evolucii organizmiv 24 (August 30, 2019): 147–53. http://dx.doi.org/10.7124/feeo.v24.1128.
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Aim. To determine the change in the structure of the inzucht-offspring in the content of cannabinoid substances in plants of different varieties of hemp under the influence of directed plus and minus selections. Methods. Taking into account the lability of natural phenol-cannabinoids, their transformation and isomerization under the influence of various factors, the method of thin-layer chromatography (TLC) was used. Plants of varieties YuSO1 and Hlyana at the budding period were labeled and separated. Results. By selecting plants in inzucht offsprings for three years aimed at reducing the content of cannabinoids in the hemp straw YSO 1 and increasing the amount of these substances in the Hlyana variety showed that the increase in the content of cannabinoids was more active than reduction, indicating a dominant feature of cannabinoids. Under the condition of isolation, self-pollination and regardless of the plus and minus selections for the content of cannabinoids, for three generations there was a decrease in plant height and sterility of varieties. Conclusions. The results of chromatographic analyzes of inzucht generations by the content of cannabinoid substances under the influence of minus and plus selections indicate their dominant feature. Regardless of the minus and plus selections by the content of cannabinoids, provided that the isolation and self-pollination were carried out, the plant height declined.
Keywords: THC, CBD, CBN, CBDА, THCA.
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Napiroon, Tiwtawat, Keerati Tanruean, Pisit Poolprasert, Markus Bacher, Henrik Balslev, Manop Poopath, and Wichai Santimaleeworagun. "Cannabinoids from inflorescences fractions of Trema orientalis (L.) Blume (Cannabaceae) against human pathogenic bacteria." PeerJ 9 (May 13, 2021): e11446. http://dx.doi.org/10.7717/peerj.11446.
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Background Cannabinoids; tetrahydrocannabinol (THC), cannabidiol (CBD) and cannabinol (CBN), might show antibacterial activity. Trema orientalis is a species in the Cannabaceae that is closely related to Cannabis through plastome phylogenetic evidence. This species is widely distributed throughout tropical Asia and is used as traditional medicine, particularly for the treatment of infectious diseases. However, no studies on the antibacterial activity of cannabinoid-containing inflorescences extracts are available. Thus, the aim of this study was to determine cannabinoid content and antibacterial activity of inflorescences fractions from T. orientalis native to Thailand. Methods We hypothesized that inflorescences from T. orientalis might display cannabinoids similar to Cannabis because of their close taxonomic relationship. We extracted the mature inflorescences and infructescence of T. orientalis in three disparate populations from different Thailand floristic regions. Extractions were subsequently partitioned into hydrophilic and lipophilic fractions using distilled water and chloroform. The lipophilic extracts were further fractionated by the column chromatography with gradient elution and analyzed by gas chromatography-mass spectrometry (GC-MS). Characterized cannabinoids were used in bioassays with multidrug-resistance bacteria. Results Lipophilic extracts and fractions of inflorescences from all Thailand floristic regions consistently displayed cannabinoids (THC, CBD and CBN) in various quantities. These extracts exhibited inhibitory activity for Staphylococcus aureus, Pseudomonas aeruginosa, and Acinetobacter baumannii strains with minimum inhibitory concentration values varying from 31.25 to 125 µg/mL. Conclusion Our study is the first to report cannabinoid detection in extracts from inflorescences of T. orientalis, a species in the Cannabaceae. These extracts and their fractions containing cannabinoids showed pronounced antibacterial activity. The use of analytic methods also demonstrated reproducible cannabinoid extraction.
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Twitchell, W., S. Brown, and K. Mackie. "Cannabinoids Inhibit N- and P/Q-Type Calcium Channels in Cultured Rat Hippocampal Neurons." Journal of Neurophysiology 78, no. 1 (July 1, 1997): 43–50. http://dx.doi.org/10.1152/jn.1997.78.1.43.
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Twitchell, W., S. Brown, and K. Mackie. Cannabinoids inhibit N- and P/Q-type calcium channels in cultured rat hippocampal neurons. J. Neurophysiol. 78: 43–50, 1997. Cannabinoids and their analogues have been found to inhibit N- and P/Q-type Ca2+ currents in cell lines and sympathetic neurons transfected with cannabinoid CB1 receptor. However, the effects of cannabinoids on Ca2+ currents in the CNS are largely unexplored. In this study we investigated whether these compounds inhibit Ca2+ channels in cultured rat hippocampal neurons. With the use of antibodies directed against the amino-terminus of the CB1 receptor, we found that in 5-day cultures pyramidally shaped neurons expressed somatic CB1 receptors, whereas in 4-wk cultures the receptor was predomintely located on neurites. In early cultures, the cannabimimetic WIN 55,212-2 reversibly inhibited whole cell Ba2+ current in a concentration-dependent ( K 1/2 = 21 nM) and pertussis-toxin-sensitive fashion. Inhibition was reduced by the CB1 antagonist SR141716. The current was unaffected by the nonpsychoactive enantiomer WIN 55,212-3. Maximal inhibition by the nonclassical cannabinoid agonist CP 55,940 and by an endogenous cannabinoid, anandamide, were similar to that seen with maximal concentrations of WIN 55,212-2. The Ba2+ current modulated by cannabinoids was carried by N-type (ω-conotoxin-GVIA-sensitive) and P/Q-type (ω-conotoxin-MVIIC-sensitive) channels. These results demonstrate cannabinoid-receptor-mediated inhibition of distinct Ca2+ channels in central neurons. Because the channels that underlie these currents are chiefly located presynaptically, and are required for evoked neurotransmitter release, our results suggest a major role for cannabinoids (endogenous and exogenous) in the modulation of synaptic transmission at CNS synapses.
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Vásquez, Clemente, Ricardo A. Navarro-Polanco, Miguel Huerta, Xóchitl Trujillo, Felipa Andrade, Benjamín Trujillo-Hernández, and Leonardo Hernández. "Effects of cannabinoids on endogenous K+ and Ca2+ currents in HEK293 cells." Canadian Journal of Physiology and Pharmacology 81, no. 5 (May 1, 2003): 436–42. http://dx.doi.org/10.1139/y03-055.
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Effects of cannabinoids on endogenous potassium and calcium currents in HEK293 cells were studied using the whole-cell variant of the patch-clamp technique. The cannabinoid agonists WIN 55,212-2, methanandamide, and anandamide (1 μM) decreased the calcium current by 53.1 ± 2.6, 47.5 ± 1.2, and 38.8 ± 3.1%, respectively, after transfection of human CB1 cannabinoid receptor (hCB1) cDNA into HEK293 cells. The delayed rectifier-like current was not changed after application of these agonists, but the inward rectifier was increased by 94.0 ± 3.6, 83.7 ± 5.1, and 63.0 ± 2.5% after application of WIN 55,212-2, methanandamide, and anandamide, respectively. The effects of the cannabinoid antagonists (AM251, AM281, and AM630) on the inward rectifier and calcium currents were the opposite of those seen with cannabinoid agonists; thus, these compounds act as inverse agonists in this preparation. These results suggest that endogenous inward rectifier and calcium currents are modulated by cannabinoids in HEK293 cells, and that some expressed receptors may be constitutively active.Key words: cannabinoids, WIN 55,212-2, anandamide, methanandamide, inverse agonists.
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Puighermanal, Emma, Arnau Busquets-Garcia, Rafael Maldonado, and Andrés Ozaita. "Cellular and intracellular mechanisms involved in the cognitive impairment of cannabinoids." Philosophical Transactions of the Royal Society B: Biological Sciences 367, no. 1607 (December 5, 2012): 3254–63. http://dx.doi.org/10.1098/rstb.2011.0384.
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Exogenous cannabinoids, such as delta9-tetrahydrocannabinol (THC), as well as the modulation of endogenous cannabinoids, affect cognitive function through the activation of cannabinoid receptors. Indeed, these compounds modulate a number of signalling pathways critically implicated in the deleterious effect of cannabinoids on learning and memory. Thus, the involvement of the mammalian target of rapamycin pathway and extracellular signal-regulated kinases, together with their consequent regulation of cellular processes such as protein translation, play a critical role in the amnesic-like effects of cannabinoids. In this study, we summarize the cellular and molecular mechanisms reported in the modulation of cognitive function by the endocannabinoid system.
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Smith, Paul F., and Yiwen Zheng. "Cannabinoids, cannabinoid receptors and tinnitus." Hearing Research 332 (February 2016): 210–16. http://dx.doi.org/10.1016/j.heares.2015.09.014.
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Laudanski, Krzysztof, and Justin Wain. "Considerations for Cannabinoids in Perioperative Care by Anesthesiologists." Journal of Clinical Medicine 11, no. 3 (January 22, 2022): 558. http://dx.doi.org/10.3390/jcm11030558.
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Increased usage of recreational and medically indicated cannabinoid compounds has been an undeniable reality for anesthesiologists in recent years. These compounds’ complicated pharmacology, composition, and biological effects result in challenging issues for anesthesiologists during different phases of perioperative care. Here, we review the existing formulation of cannabinoids and their biological activity to put them into the context of the anesthesia plan execution. Perioperative considerations should include a way to gauge the patient’s intake of cannabinoids, the ability to gain consent properly, and vigilance to the increased risk of pulmonary and airway problems. Intraoperative management in individuals with cannabinoid use is complicated by the effects cannabinoids have on general anesthetics and depth of anesthesia monitoring while simultaneously increasing the potential occurrence of intraoperative hemodynamic instability. Postoperative planning should involve higher vigilance to the risk of postoperative strokes and acute coronary syndromes. However, most of the data are not up to date, rending definite conclusions on the importance of perioperative cannabinoid intake on anesthesia management difficult.
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Ellert-Miklaszewska, Aleksandra, Iwona Anna Ciechomska, and Bozena Kaminska. "Synthetic Cannabinoids Induce Autophagy and Mitochondrial Apoptotic Pathways in Human Glioblastoma Cells Independently of Deficiency in TP53 or PTEN Tumor Suppressors." Cancers 13, no. 3 (January 22, 2021): 419. http://dx.doi.org/10.3390/cancers13030419.
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Glioblastomas (GBMs) are aggressive brain tumors with frequent genetic alterations in TP53 and PTEN tumor suppressor genes rendering resistance to standard chemotherapeutics. Cannabinoid type 1 and 2 (CB1/CB2) receptor expression in GBMs and antitumor activity of cannabinoids in glioma cells and animal models, raised promises for a targeted treatment of these tumors. The susceptibility of human glioma cells to CB2-agonists and their mechanism of action are not fully elucidated. We determined CB1 and CB2 expression in 14 low-grade and 21 high-grade tumor biopsies, GBM-derived primary cultures and established cell lines. The non-selective CB receptor agonist WIN55,212-2 (but not its inactive enantiomer) or the CB2-selective agonist JWH133 induced apoptosis in patient-derived glioma cultures and five established glioma cell lines despite p53 and/or PTEN deficiency. Growth inhibitory efficacy of cannabinoids correlated with CB1/CB2 expression (EC50 WIN55,212-2: 7.36–15.70 µM, JWH133: 12.15–143.20 µM). Treatment with WIN55,212-2 or JWH133 led to activation of the apoptotic mitochondrial pathway and DNA fragmentation. Synthetic cannabinoid action was associated with the induction of autophagy and knockdown of autophagy genes augmented cannabinoid-induced apoptotic cell death. The high susceptibility of human glioblastoma cells to synthetic cannabinoids, despite genetic defects contributing to apoptosis resistance, makes cannabinoids promising anti-glioma therapeutics.
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Koay, Luan C., Rachael J. Rigby, and Karen L. Wright. "Cannabinoid-induced autophagy regulates suppressor of cytokine signaling-3 in intestinal epithelium." American Journal of Physiology-Gastrointestinal and Liver Physiology 307, no. 2 (July 15, 2014): G140—G148. http://dx.doi.org/10.1152/ajpgi.00317.2013.
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Autophagy is a catabolic process involved in homeostatic and regulated cellular protein recycling and degradation via the lysosomal degradation pathway. Emerging data associate impaired autophagy, increased activity in the endocannabinoid system, and upregulation of suppressor of cytokine signaling-3 (SOCS3) protein expression during intestinal inflammation. We have investigated whether these three processes are linked. By assessing the impact of the phytocannabinoid cannabidiol (CBD), the synthetic cannabinoid arachidonyl-2′-chloroethylamide (ACEA), and the endocannabinoid N-arachidonoylethanolamine (AEA) on autophagosome formation, we explored whether these actions were responsible for cyclic SOCS3 protein levels. Our findings show that all three cannabinoids induce autophagy in a dose-dependent manner in fully differentiated Caco-2 cells, a model of mature intestinal epithelium. ACEA and AEA induced canonical autophagy, which was cannabinoid type 1 receptor-mediated. In contrast, CBD was able to bypass the cannabinoid type 1 receptor and the canonical pathway to induce autophagy, albeit to a lesser extent. Functionally, all three cannabinoids reduced SOCS3 protein expression, which was reversed by blocking early and late autophagy. In conclusion, the regulatory protein SOCS3 is regulated by autophagy, and cannabinoids play a role in this process, which could be important when therapeutic applications for the cannabinoids in inflammatory conditions are considered.
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An, Dongchen, Steve Peigneur, Louise Antonia Hendrickx, and Jan Tytgat. "Targeting Cannabinoid Receptors: Current Status and Prospects of Natural Products." International Journal of Molecular Sciences 21, no. 14 (July 17, 2020): 5064. http://dx.doi.org/10.3390/ijms21145064.
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Cannabinoid receptors (CB1 and CB2), as part of the endocannabinoid system, play a critical role in numerous human physiological and pathological conditions. Thus, considerable efforts have been made to develop ligands for CB1 and CB2, resulting in hundreds of phyto- and synthetic cannabinoids which have shown varying affinities relevant for the treatment of various diseases. However, only a few of these ligands are clinically used. Recently, more detailed structural information for cannabinoid receptors was revealed thanks to the powerfulness of cryo-electron microscopy, which now can accelerate structure-based drug discovery. At the same time, novel peptide-type cannabinoids from animal sources have arrived at the scene, with their potential in vivo therapeutic effects in relation to cannabinoid receptors. From a natural products perspective, it is expected that more novel cannabinoids will be discovered and forecasted as promising drug leads from diverse natural sources and species, such as animal venoms which constitute a true pharmacopeia of toxins modulating diverse targets, including voltage- and ligand-gated ion channels, G protein-coupled receptors such as CB1 and CB2, with astonishing affinity and selectivity. Therefore, it is believed that discovering novel cannabinoids starting from studying the biodiversity of the species living on planet earth is an uncharted territory.