Relevant bibliographies by topics / Drug receptors

Academic literature on the topic 'Drug receptors'

Author: Grafiati
Published: 4 June 2021
Last updated: 26 July 2024

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles

Select a source type:

Contents

Consult the lists of relevant articles, books, theses, conference reports, and other scholarly sources on the topic 'Drug receptors.'

Next to every source in the list of references, there is an 'Add to bibliography' button. Press on it, and we will generate automatically the bibliographic reference to the chosen work in the citation style you need: APA, MLA, Harvard, Chicago, Vancouver, etc.

You can also download the full text of the academic publication as pdf and read online its abstract whenever available in the metadata.

Journal articles on the topic "Drug receptors"

1

Shaw, P., and L. S. Pilowsky. "Probing Cortical Sites of Antipsychotic Drug Action within vivoReceptor Imaging." Behavioural Neurology 12, no. 1-2 (2000): 3–9. http://dx.doi.org/10.1155/2000/184707.

Full text
Abstract:
Imaging receptors using radioactive ligands has allowed direct determination of the sites of action of antipsychotic drugs. Initial studies relating antipsychotic drug efficacy to action at striatal dopamine D2-like receptors have recently been undermined. Developments in imaging extrastriatal dopamine D2-like receptors suggest rather that antagonism of these receptors in the temporal cortex is the common site of action for antipsychotic drugs, with occupancy at striatal receptors relating more closely to extrapyramidal side effects. Further work into dopamine receptor subtypes and other receptor groups such as serotonin and GABA neurotransmitters awaits the development of suitable probes, but there are some initial finding. Again a main site of antipsychotic drug action is at cortical levels with high degrees of cortical D1 and 5HT2areceptor occupancy attained particularly by atypical antipsychotic drugs.
APA, Harvard, Vancouver, ISO, and other styles
2

Hartig, Paul R. "Can cloned receptors aid drug research?" Proceedings of the Royal Society of Edinburgh. Section B. Biological Sciences 99, no. 1-2 (1992): 19–25. http://dx.doi.org/10.1017/s0269727000013014.

Full text
Abstract:
Synopsis:Over 50 different neurotransmitter and hormone receptors have been cloned, transfected and characterised. Within the pharmaceutical industry, the thrust of this research is now moving from receptor cloning to focussed application of these new tools to the task of drug development. With human receptor clones now available, it is possible to target drug design to single human proteins from the inception of a drug-design project. A critical question is whether human genes will express a human pharmacology when expressed in non-human, non-neuronal cell lines. Relevant results from studies with the human serotonin 5-HT2 and 5-HT1D receptors are presented, including the cloning of a rat 5-HT1B receptor which is homologous to a human 5-HT1D receptor gene. Another issue is the relationship between agonist and antagonist binding sites. The ability to study individual human receptors in selected cell lines which are free from interfering receptors has helped to advance our understanding of this relationship. Studies comparing agonist and antagonist binding sites of the human 5-HT2 receptor are described. Finally, the fact that so many neurotransmitter receptors belong to the same gene superfamily, the G-protein-coupled or 7TM (7 transmembrane domain) receptor superfamily, allows us to form new insights about receptor structure and function. Examples where comparative studies of gene sequences are helping to predict pharmacological properties of drugs are described.
APA, Harvard, Vancouver, ISO, and other styles
3

Takayanagl, Issei. "Drug receptors and drug design." Japanese Journal of Pharmacology 67 (1995): 45. http://dx.doi.org/10.1016/s0021-5198(19)46150-7.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Sunahara, Roger K., Philip Seeman, Hubert H. M. Van Tol, and Hyman B. Niznik. "Dopamine Receptors and Antipsychotic Drug Response." British Journal of Psychiatry 163, S22 (December 1993): 31–38. http://dx.doi.org/10.1192/s000712500029257x.

Full text
Abstract:
Dopamine receptors have been divided into two major types – D1 and D2 – based primarily on pharmacological and biochemical criteria. Recent advances in the molecular biology of the dopamine receptor system have allowed the identification and characterisation of at least five distinct neuronal dopamine receptor genes (D1 to D5). These genes encode dopamine receptors belonging to the D1 receptor family, termed D1 and D5, and three D2-like receptors, termed D2, D3 and D4. These receptors are distinguished on the basis of their primary structure, chromosomal location, mRNA size and tissue distribution, and biochemical and pharmacological differences. Although individually these receptor subtypes may not be directly and exclusively involved in the maintenance or expression of schizophrenia, alterations of any of the receptors may contribute to the perturbation or instability of dopaminergic homeostasis in the brain. What was once thought to be a simple two-receptor system seems to have emerged as an intricate and interactive entity. This review summarises what is currently understood about dopamine receptors, their role in antipsychotic drug action, and their association with psychosis.
APA, Harvard, Vancouver, ISO, and other styles
5

García-Nafría, Javier, and Christopher G. Tate. "Cryo-Electron Microscopy: Moving Beyond X-Ray Crystal Structures for Drug Receptors and Drug Development." Annual Review of Pharmacology and Toxicology 60, no. 1 (January 6, 2020): 51–71. http://dx.doi.org/10.1146/annurev-pharmtox-010919-023545.

Full text
Abstract:
Electron cryo-microscopy (cryo-EM) has revolutionized structure determination of membrane proteins and holds great potential for structure-based drug discovery. Here we discuss the potential of cryo-EM in the rational design of therapeutics for membrane proteins compared to X-ray crystallography. We also detail recent progress in the field of drug receptors, focusing on cryo-EM of two protein families with established therapeutic value, the γ-aminobutyric acid A receptors (GABAARs) and G protein–coupled receptors (GPCRs). GABAARs are pentameric ion channels, and cryo-EM structures of physiological heteromeric receptors in a lipid environment have uncovered the molecular basis of receptor modulation by drugs such as diazepam. The structures of ten GPCR–G protein complexes from three different classes of GPCRs have now been determined by cryo-EM. These structures give detailed insights into molecular interactions with drugs, GPCR–G protein selectivity, how accessory membrane proteins alter receptor–ligand pharmacology, and the mechanism by which HIV uses GPCRs to enter host cells.
APA, Harvard, Vancouver, ISO, and other styles
6

Suvarna, B. S. "Drug - Receptor Interactions." Kathmandu University Medical Journal 9, no. 3 (June 13, 2012): 203–7. http://dx.doi.org/10.3126/kumj.v9i3.6306.

Full text
Abstract:
In present-day pharmacology and medicine, it is usually taken for granted that cells contain a host of highly specific receptors. Drugs act on the cell membrane by physical and/or chemical interactions. This is usually through specific drug receptor sites known to be located on the membrane. These are defined as proteins on or within the cell that bind with specificity to particular drugs, chemical messenger substances or hormones and mediate their effects on the body. Today, the concept of specific receptors for drugs and transmitters lies at the very heart of pharmacology. However, it is only relatively recently that the notion of drug-specific receptors has become widely accepted, with considerable doubts being expressed about their existence as late as the 1960s.DOI: http://dx.doi.org/10.3126/kumj.v9i3.6306 Kathmandu Univ Med J 2011;9(3):203-7
APA, Harvard, Vancouver, ISO, and other styles
7

Kondej, Magda, Piotr Stępnicki, and Agnieszka A. Kaczor. "Multi-Target Approach for Drug Discovery against Schizophrenia." International Journal of Molecular Sciences 19, no. 10 (October 10, 2018): 3105. http://dx.doi.org/10.3390/ijms19103105.

Full text
Abstract:
Polypharmacology is nowadays considered an increasingly crucial aspect in discovering new drugs as a number of original single-target drugs have been performing far behind expectations during the last ten years. In this scenario, multi-target drugs are a promising approach against polygenic diseases with complex pathomechanisms such as schizophrenia. Indeed, second generation or atypical antipsychotics target a number of aminergic G protein-coupled receptors (GPCRs) simultaneously. Novel strategies in drug design and discovery against schizophrenia focus on targets beyond the dopaminergic hypothesis of the disease and even beyond the monoamine GPCRs. In particular these approaches concern proteins involved in glutamatergic and cholinergic neurotransmission, challenging the concept of antipsychotic activity without dopamine D2 receptor involvement. Potentially interesting compounds include ligands interacting with glycine modulatory binding pocket on N-methyl-d-aspartate (NMDA) receptors, positive allosteric modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, positive allosteric modulators of metabotropic glutamatergic receptors, agonists and positive allosteric modulators of α7 nicotinic receptors, as well as muscarinic receptor agonists. In this review we discuss classical and novel drug targets for schizophrenia, cover benefits and limitations of current strategies to design multi-target drugs and show examples of multi-target ligands as antipsychotics, including marketed drugs, substances in clinical trials, and other investigational compounds.
APA, Harvard, Vancouver, ISO, and other styles
8

Sonoda, J., and R. M. Evans. "Biological function and mode of action of nuclear xenobiotic receptors." Pure and Applied Chemistry 75, no. 11-12 (January 1, 2003): 1733–42. http://dx.doi.org/10.1351/pac200375111733.

Full text
Abstract:
Two related nuclear receptors, the pregnane X receptor (PXR) and the constitutive androstane receptor (CAR), act as xenobiotic sensors that protect the body from a multitude of foreign chemicals (xenobiotics) and play a central role in the metabolism and clearance of steroids and toxic endogenous lipids (endobiotics). A structurally diverse array of chemicals including pharmaceutical drugs, steroids, herbal extracts, and pesticides activate PXR or CAR. This activation results in induction of overlapping, but yet distinct drug clearance pathways consisting of cytochrome P450 enzymes, conjugating enzymes, drug transporters, and other related proteins. Similar pathways are also utilized to protect the body from toxic compounds of endogenous origin. Thus, the xenobiotic regulatory circuit contributes both to drug-drug and food-drug interactions as well as endocrine disruption. Consistent with the notion that xenobiotic receptors regulate drug clearance, single nucleotide polymorphisms (SNPs) in either the receptors themselves or receptor-binding sites in the regulatory region of genes encoding metabolic enzymes appear to contribute to the polymorphic expression of components of drug clearance pathways. Together, the xenobiotic receptors PXR and CAR confer metabolic immunity via the ability to control an integrated array of target genes.
APA, Harvard, Vancouver, ISO, and other styles
9

Parker, E. M., and D. W. Smith. "G Protein-Coupled Serotonin Receptors-Multiple Subtypes, Multiple Opportunities." Current Pharmaceutical Design 1, no. 3 (October 1995): 363–72. http://dx.doi.org/10.2174/1381612801666220918170118.

Full text
Abstract:
Serotonin receptors have been fertile targets for drug development for decades. The attractiveness of serotonin receptors as drug targets is due to the wide range of physiological processes in which serotonin plays a role and to diversity of receptor subtypes that mediate the physiological effects of serotonin. The powerful combination of molecular cloning and pharmacology has thus far led to the identification of fifteen different serotonin receptor subtypes. Fourteen of these serotonin receptors are G protein­ coupled receptors and one is a ligand-gated ion channel. Because many of these serotonin receptor subtypes have been identified very recently, the current opportunities for development of d gs that act via these receptors are manifold. This chapter focuses on recent molecular insights into the structure and function of serotonin receptors, discusses the relevance of these insights to the design and discovery of receptor selective drugs and reviews recently discovered selective antagonists for serotonin receptors.
APA, Harvard, Vancouver, ISO, and other styles
10

Reynolds, Gavin P., and Olga O. McGowan. "Mechanisms underlying metabolic disturbances associated with psychosis and antipsychotic drug treatment." Journal of Psychopharmacology 31, no. 11 (September 11, 2017): 1430–36. http://dx.doi.org/10.1177/0269881117722987.

Full text
Abstract:
The increase in cardiovascular disease and reduced life expectancy in schizophrenia likely relate to an increased prevalence of metabolic disturbances. Such metabolic risk factors in schizophrenia may result from both symptom-related effects and aetiological factors. However, a major contributory factor is that of treatment with antipsychotic drugs. These drugs differ in effects on body weight; the underlying mechanisms are not fully understood and may vary between drugs, but may include actions at receptors associated with the hypothalamic control of food intake. Evidence supports 5-hydroxytryptamine receptor 2C and dopamine D2 receptor antagonism as well as antagonism at histamine H1 and muscarinic M3 receptors. These M3 receptors may also mediate the effects of some drugs on glucose regulation. Several antipsychotics showing little propensity for weight gain, such as aripiprazole, have protective pharmacological mechanisms, rather than just the absence of a hyperphagic effect. In addition to drug differences, there is large individual variation in antipsychotic drug-induced weight gain. This pharmacogenetic association reflects genetic variation in several drug targets, including the 5-hydroxytryptamine receptor 2C, as well as genes involved in obesity and metabolic disturbances. Thus predictive genetic testing for drug-induced weight gain would represents a first step towards personalised medicine addressing this severe and problematic iatrogenic disease.
APA, Harvard, Vancouver, ISO, and other styles
More sources

Dissertations / Theses on the topic "Drug receptors"

1

Wright, Sherie Rose. "The role of A2A receptors in drug addiction: interaction with mGIu5 receptors." Thesis, University of Surrey, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.583347.

Full text
Abstract:
The mechanism by which the adenosine A2A receptor mediates the actions of multiple drugs of abuse is thought to be partly attributable to interactions with dopamine D2 receptors in the striatum; a key structure in drug-related reward, reinforcement and motor responses. Evidence now suggests that this interaction could be further influenced by actions of the metabotropic glutamate receptor, mGlu5, which is co- expressed with striatal A2A and D2 receptors. This work aimed to identify the role of A2A receptors in mediating the locomotor and stereotypic responses to chronic administration of cocaine, morphine and methamphetamine with the use of wild-type (WT) and adenosine A2A receptor knockout (KO) mice. Further, via quantitative autoradiography in WT and A2A KO mice, the experiments described in this thesis also investigated whether the A2A receptor was involved in the regulation of D2 and mGlu5, receptor binding, both under physiological conditions and following chronic cocaine, morphine and methamphetamine administration. A significant reduction of mGlu5, but not D2 receptor density was observed in the ventral striatum of treatment-naive A2A KO mice, giving further evidence for the presence of a striatal A2A-mGlu5 interaction at the receptor level. Chronic administration of methamphetamine, but not cocaine or morphine, caused a significant upregulation of striatal mGlu5, receptors in WT mice. This was accompanied by the manifestation of a stereotypic rearing behaviour in methamphetamine-treated WT mice, both of which were completely abolished in A2A KO mice, suggesting a drug-specific role of an A2A- mGlu5 receptor interaction in the methamphetamine-induced rearing response. Furthermore, the combination of sub-threshold doses of A2A and mGlu5, receptor antagonists significantly attenuated methamphetamine-induced rearing in WT mice, confirming that a striatal A2A-niGlus interaction was specifically involved in the mediation of this response. Chronic morphine treatment caused an upregulation of thalamic mGlu5 receptors in A2A KO mice, indicating that an A2A-mGlus interaction may also be of relevance in the mediation of morphine-induced antinociceptive tolerance. No changes in D2 receptor binding were observed in either treatment-naive WT or A2A KO mice, or those mice treated chronically with cocaine, morphine or methamphetamine, suggesting that the A2A receptor is not involved in modulating the receptor density of D2 receptors either physiologically, or following chronic drug administration. Collectively, the results described in this thesis show that the contribution of the A2A receptor in mediating the locomotor and stereotypic responses to chronic drug administration is drug-dependent, as is the ability of A2A to regulate mGlu5 receptor binding. Specifically, the therapeutic relevance of the novel A2A-mGlus interaction identified following chronic methamphetamine administration merits further investigation, as it adds to a growing body of evidence which suggest simultaneous targeting of A2A and mGlu5 receptors has implications for the improved efficacy of treatments of basal ganglia disorders and drug addiction.
APA, Harvard, Vancouver, ISO, and other styles
2

Morizzo, Erika. "G Protein-Coupled Receptors as Potential Drug Target: From Receptor Topology to Rational Drug Design, an in-silico Approach." Doctoral thesis, Università degli studi di Padova, 2009. http://hdl.handle.net/11577/3426081.

Full text
Abstract:
G protein-coupled receptors (GPCRs) constitute a very large family of heptahelical, integral membrane proteins that mediate a wide variety of physiological processes, ranging from the transmission of the light and odorant signals to the mediation of neurotransmission and hormonal actions. GPCRs are dysfunctional or deregulated in several human diseases and are estimated to be the target of more than 40% of drugs used in clinical medicine today. The crystal structures of rhodopsin and the recent published crystal structures of beta-adrenergic receptors and human A2A Adrenergic Receptor provide the information of the three-dimensional structure of GPCRs, which supports homology modeling studies and structure-based drug-design approaches. Rhodopsin-based homology modeling has represented for many years a widely used approach to built GPCR three-dimensional models. Structural models can be used to describe the interatomic interactions between ligand and receptor and how the binding information is transmitted through the receptor. Both agonist and antagonist like states can be described by several different conformational receptor states depending on the nature of both ligand and receptor. Considering different complementarities, we might explore different conformations of the same pharmacological state. We investigated the molecular pharmacology of adenosine receptors and, in particular, the human A3 adenosine receptor (hA3AR) by using an interdisciplinary approach to speed up the discovery and structural refinement of new potent and selective hA3AR antagonists. Human A3AR belongs to adenosine receptors family of GPCRs, which consists of four distinct subtypes: A1, A2A, A2B, A3 that are ubiquitously expressed in the human body. The hA3AR, which is the most recently identified adenosine receptor, is implicated in a variety of important physiological processes. Activation of A3ARs increases the release of inflammatory mediators, such as histamine from rodent mast cells, and it inhibits the production of tumor necrosis factor-alpha. The activation of the hA3AR seems to be involved in immunosuppression and in the response to ischemia of the brain and heart. Agonists or antagonists of A3ARs are potential therapeutic agents for the treatment of ischemic and inflammatory diseases. The first model of human A3AR has been built using a conventional rhodopsin-based homology modeling approach. The model has been used to probe atomic level specific interactions, detected using site-directed mutagenesis analysis. The rhodopsin-based model of the hA3AR in its resting state (antagonist-like state) has been revisited, taking into account a novel strategy to simulate the possible receptor reorganization induce by the antagonist-binding. We called this new strategy ligand-based homology modeling (LBHM). It is an evolution of a conventional homology modeling algorithm: any selected atoms will be included in energy tests and in minimization stages of the modeling procedure. Ligand-based option is very useful when one wishes to build a homology model in the presence of a ligand docked to the primary template. Starting from the conventional rhodopsin-based homology model and applying our ligand-based homology modeling implementation we can generate other antagonist-like conformational states of hA3AR in which the ligand recognition cavity is expanded. Using different antagonist-like conformational states, we are able to rationalize the observed activities for all the compounds analyzed. Many severe analysis concerning false-positives and false-negatives situations are usually conducted. To strictly validate this methodology as novel tool to address the multi-conformational space of GPCRs, we have analyzed different classes of known human A3 antagonists in the corresponding putative ligand binding site: for example triazoloquinoxalin-1-one derivatives, arylpyrazolo-quinoline derivatives and pyrazolo-triazolo-pyrimidines derivatives. These studies led to the identification of groups for every class of antagonists that, introduced one by one in a suitable position, afford high hA3AR affinity and good selectivity. Starting from these binding requirements, we decided to perform an in silico molecular simplification approach to identify a suitable fragmentation route of the 4-amino-triazoloquinoxalin-1-one scaffold and explore which of the structural features were essential to guarantee efficient ligand-receptor recognition. With the availability of new three dimensional templates different from rhodopsin, we built new models of hA3AR. All the models were used for a molecular dynamic simulation in a POPC bilayer to investigate the topological fluctuation of the binding pocket.
I recettori accoppiati alle proteine G (GPCR) costituiscono una grande famiglia di proteine integrali di membrana caratterizzate da sette eliche transmenmbrana, che mediano un'ampia gamma di processi fisiologici che vanno dalla trasmissione della luce e dei segnali olfattivi alla mediazione della neurotrasmissione e dell'azione degli ormoni. I GPCR mancano di una corretta regolazione in molte patologie umane ed è stato stimato che costituiscano il target del 40% dei medicinali utilizzati attualmente in clinica. La struttura cristallografica della rodopsina e le strutture più recenti del recettore beta adrenergico e del recettore adenosinico A2A forniscono l'informazione strutturale che sta alla base della costruzione di modelli per omologia e degli approcci di structure-based drug design dei GPCR. La costruzione di modelli di GPCR per omologia basati sulla struttura della rodopsina ha rappresentato per molti anni un approccio ampiamente utilizzato. Questi modelli possono essere usati per descrivere le interazioni interatomiche tra ligando e recettore e come le informazioni sono trasmesse attraverso il recettore. Diversi stati conformazionali del recettore possono essere in grado di descrivere la conformazione del recettore che lega l'agonista e quella che lega l'antagonista, a seconda della natura di ligando e recettore. Se si considerano diverse complementarietà, si possono esplorare diversi stati conformazionali di uno stesso stato farmacologico. Noi abbiamo studiato la farmacologia molecolare dei recettori adenosinici e, in particolare, del recettore adenosinico A3 umano (hA3AR), utilizzando un approccio interdisciplinare al fine di massimizzare la scoperta e l'ottimizzazione strutturale di nuovi antagonisti potenti e selettivi per il hA3AR. Il hA3AR fa parte della famiglia dei recettori adenosinici che consiste in quattro diversi sottotipi (A1, A2A, A2B, A3) che sono espressi in tutto il corpo umano. Il recettore adenosinico A3 è stato identificato più recentemente ed è implicato in importanti processi fisologici. L'attivazione del hA3AR aumenta il rilascio di mediatori dell'infiammazione, come l'istamina dalle mastcellule, e inibisce la produzione del TNF-alpha. L'attivazione del hA3AR sembra essere coinvolta nell'immunosoppressione e nella risposta ischemica di cuore e cervello. Agonisti o antagonisti del hA3AR sono potenziali agenti terapeutici nel trattamento di patologie ischemiche e infiammatorie. Il primo modello di hA3AR è stato costruito usando un approccio convenzionale di homology modeling basato sulla rodopsina ed è nel suo stato che lega l'antagonista. Dopo essere stato utilizzato per verificare le interazioni a livello molecolare che erano state evidenziate da studi di mutagenesi, il modello è stato rivisto prendendo in considerazione una nuova strategia che simula la possibile riorganizzazione del recettore indotta dal legame con l'antagonista. Abbiamo chiamato questa strategia ligand-based homology modeling. E' un'evoluzione dell'algoritmo convenzionale di homology modeling: ogni atomo selezionato viente preso in considerazione nei test energetici e nelle fasi di minimizzazione della procedura di modeling. L'opzione ligand-based è molto utile quando si vuole costruire un modello per omologia in presenza di un ligando nella sua ipotetica conformazione di legame nel templato iniziale. A partire dal modello ottenuto dalla rodopsina e applicando la tecnica del LBHM, possiamo generare altri stati conformazionali del recettore hA3AR che legano l'antagonista, nei quali la cavità di riconoscimento del ligando è espansa. Usando diversi stati conformazionali che legano l'antagonista, possiamo razionalizzare l'attività misurata sperimentalmente di tutti i composti analizzati. Sono condotte severe analisi relative a falsi positivi e falsi negativi. Per validare la metodologia come nuovo strumento per indirizzare lo spazio multiconformazionale dei GPCR, abbiamo analizzato diverse classi di antagonisti con attività nota sul hA3AR: ad esempio derivati triazolo-chinossalinonici, derivati arilpirazolo-chinolinici e derivati pirazolo-triazolo-pirimidinici. Questi studi hanno portato all'identificazione di gruppi per ogni classe di antagonisti che, se introdotti in una precisa posizione, portano ad un'alta affinità e ad una buona selettività per il hA3AR. A partire dalle caratteristiche risultate importanti per il legame, abbiamo applicato una tecnica di semplificazione molecolare in silico per identificare una possibile via di frammentazione della struttura 4-amino-triazolochinoassalin-1-onica ed esplorare quali sono le caratteristiche strutturali essenziali per garantire un'efficiente riconoscimento ligando-recettore. Con la disponibilità di nuove strutture tridimensionali da utilizzare come templati diversi dalla rodopsina, abbiamo costruito nuovi modelli del recettore hA3AR. Tutti i modelli sono stati usati per una simulazione di dinamica molecolare in un doppio strato fosfolipidico, per analizzare le fluttuazioni topologiche della tasca di legame.
APA, Harvard, Vancouver, ISO, and other styles
3

Bertilsson, Göran. "Studies on nuclear receptors involved in drug metabolism /." Stockholm, 2001. http://diss.kib.ki.se/2001/91-628-4697-3/.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Metaxas, Athanasios. "The involvement of nicotinic cholinergic receptors in drug abuse." Thesis, University of Surrey, 2010. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.520556.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Arif, Khalid. "Evaluation of hormonal receptors in breast cancer drug therapy." Thesis, University of Lincoln, 2014. http://eprints.lincoln.ac.uk/14682/.

Full text
Abstract:
Breast cancer is the most common type of cancer in women worldwide. Approximately two-thirds of breast cancers are oestrogen receptor positive (ER+), which are activated via oestrogen dependent and independent mechanisms. The pathogenic role of oestrogen in breast cancer is well established, thus, targeting ER becomes an essential target in breast cancer anti-hormonal therapy. Tamoxifen is the most important anti-hormonal therapeutic agent which has been used as the gold standard in the treatment of ER+ breast cancer patients. Tamoxifen acts by competing with oestrogen for binding to the ER and reduces the transcription of oestrogen dependent genes. However, approximately 30-50% of patients either fail to respond or eventually become resistant to tamoxifen via not fully elucidated mechanisms, resulting in a serious clinical challenge in breast cancer management. Also there is increasing evidence that cancers are driven by cancer stem cells which are characterised by their ability for self renewal and resistance to drug therapies. Therefore the aim of this study was to evaluate the role of oestrogen receptors in both de novo and acquired tamoxifen resistant breast cancer. Study the influence of stem cell factors and the embryonic stemness gene in both MDA-MB-231 and MCF7/Tmx breast cancer cell lines with respect to the hypothesis that anti-stem cell factor and silencing of the Nanog may restore sensitivity to tamoxifen and enhance cell apoptosis. Qualitative and quantitative assays showed significant expression of CD44, PgP, MRP1 and embryonic markers (Nanog, Oct3/4 and Sox2) in MDA-MB-231 and MCF7/Tmx cells. Independently, MDA-MB-231, MCF7/Tmx and parental MCF7/WT cells were treated with monoclonal anti-stem cell factor (ACSF) and interfered with Nanog short interference RNA (siRNA), then growth rate, drug accumulation and apoptosis were assessed in response to 4-hydroxtamoxifen (4-OHT). Quantitative analysis of the influx and efflux rate was performed using the Technetium (99mTc) sestamibi assay in response to blocking SCF. iv Results show a significant apoptosis enhancement after treatment with ASCF in both MDA-MB-231 and MCF/Tmx cells (P<0.005) and a significant increase in the influx rate of 99mTc-MIBI in MDA-MB-231 cells. Growth rate and apoptosis markers were assessed prior to and after the silencing of Nanog gene. Results show a significant increase in apoptosis and reduction in the growth rate in both MDA-MB-231 and MCF/Tmx cells (P<0.005). This study demonstrates that multi drug resistance is mainly a phenomenon of acquired tamoxifen resistance, but not de novo resistance. The inhibition of SCF could inhibit cell proliferation and significantly increases cell sensitivity to tamoxifen in MDA-MB-231 and acquired tamoxifen resistant cells MCF7/Tmx. This study identified a high expression of embryonic markers Nanog, Oct3/4 and Sox2 in both MDA-MB-231 and MCF7/Tmx cells and that the silencing of the Nanog gene reduces cell proliferation and increases apoptosis in MDA-MB-231 and MCF7/Tmx cells. In conclusion, the results suggest that the neutralisation of stem cell factor may play an important role in enhancing tamoxifen response in ER- cells and less in acquired tamoxifen resistant breast cancer cells, via enhancing drug accumulation. The positive association of the embryonic markers with negative (ER-) and acquired tamoxifen resistant breast cancer cells could be used as prognostic markers and the knockdown of these transcription markers could enhance the response to tamoxifen and could be used in the management of breast cancer.
APA, Harvard, Vancouver, ISO, and other styles
6

Besco, Julie Ann. "Genomic structure and alternative splicing of type R2B receptor protein tyrosine phosphatases, and the role of RPTPrho." Columbus, Ohio : Ohio State University, 2003. http://rave.ohiolink.edu/etdc/view?acc%5Fnum=osu1041353035.

Full text
Abstract:
Thesis (Ph. D.)--Ohio State University, 2003.
Title from first page of PDF file. Document formatted into pages; contains xvii, 227 p. Includes abstract and vita. Advisor: Andrej Rotter, Dept. of Pharmacology. Includes bibliographical references (p. 201-227).
APA, Harvard, Vancouver, ISO, and other styles
7

Nylander, Sven. "Thrombin/ADP-induced platelet activation and drug intervention /." Linköping : Univ, 2005. http://www.bibl.liu.se/liupubl/disp/disp2005/med885s.pdf.

Full text
APA, Harvard, Vancouver, ISO, and other styles
8

Leach, Katie. "Pharmacological analysis of the CC chemokine receptors, CCR4 and CCR5 signalling properties and receptor-drug interactions." Thesis, University of Reading, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.427859.

Full text
APA, Harvard, Vancouver, ISO, and other styles
9

Greyerz, Salome Barbara von. "Molecular aspects of drug recognition by specific T cell receptors /." [S.l.] : [s.n.], 1999. http://www.ub.unibe.ch/content/bibliotheken_sammlungen/sondersammlungen/dissen_bestellformular/index_ger.html.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Jiang, Tian. "Drug affinity and binding site signatures in extrasynaptic GABAA receptors." Thesis, The University of Sydney, 2021. https://hdl.handle.net/2123/27104.

Full text
Abstract:
GABAA receptors are ligand-gated ion channels that play vital roles in the central nervous system due to their widespread distribution and involvement in vital biochemical process. GABAA receptors that express extrasynaptically are suggested as important targets for treating disorders such as epilepsy, sleep disturbances, stress, and mood disorders. Various pharmaceutical campaigns have succeeded in developing pharmacologically and clinically important drugs for the active sites of GABAA receptors. However, as the drugs do not exclusively bind to the targeted subtypes, they are usually associated with severe side effects. Therefore, it is of great importance to explore binding pockets on extrasynaptic GABAA receptors that have the potential to be targets for subtype-selective drugs that exclusively work on extrasynaptic receptors. GABAA receptors are assembled from five subunits of four different types, with multiple promising subunit compositions. This results in many different subunit interfaces and binding sites in between subunits. In the present study, possible drug binding pockets on GABAA receptors were mapped and compared, both sequentially and structurally. The neurosteroid and general anesthetic pockets on the α4β3δ GABAA receptor were identified to be more likely targets than other pockets for the development of extrasynaptic-selective drugs. The binding sites on the homology models of GABAA receptors in the active conformation were used in the analysis throughout the thesis, as the determined sites are for positive modulators. A novel targeted molecular dynamic method was co-developed here for simulating the activation pathway of the α4β3δ GABAA receptor following the path of α1 glycine receptors, as no active conformation has been released for GABAA receptors. During protein activation an increase in the druggability of the receptor was observed, as well as movement correlations in the two determined binding sites. To stabilise the structure of α4β3δ GABAA receptor in the open conformation before investigating the binding sites in the simulation, two equilibration methods were revised and compared here. One of the methods was then chosen to equilibrate the receptor in the active state in the molecular dynamics simulation, as it performed better to keep the protein channel ion-permeable and keep the two determined binding sites stable within the simulation. Significantly, a tilting caused by H-bonds between the β3 and δ subunit was observed during the simulations after equilibration by both methods, which could affect the drug binding to δ-containing GABAA receptors. Finally, promising sites and binding modes for THDOC and DS2 on α4β3δ GABAA receptor were investigated using molecular docking and molecular dynamics simulations. Residues that form stable contacts with ligands were identified, which offer mutation targets for further confirmation of binding sites. The δN318 residue is suggested here as the key residue that contributes to the favorable binding energy of THDOC on δ+β3– interface, which agrees with the experimental result that THDOC shows a dramatically higher modulation effect on δ-containing receptors than those without the δ subunit. This offers the opportunity to develop δ-selective drugs based on the molecular structure of THDOC. Together these results provide important new information about drug binding sites in GABAA receptors for developing extrasynaptic-selective drugs for treating epilepsy, sleep disturbances, stress, and mood disorders with minimum side effects. The contributions including information about the binding pockets and unique residues that are potential targets for designing extrasynaptic-selective drugs was identified. The promising binding pockets and binding modes for two drug molecules – THDOC and DS2 was also investigated. Furthermore, novel methodologies have been provided in this thesis for investigating drug binding sites in different conformations and for exploring the activation pathway of GABAA receptors. These methodologies could further be used as tools for understanding the selectivity and druggability of binding sites, simulating the conformational transition pathway, and exploring the subtype-selective drugs on other proteins.
APA, Harvard, Vancouver, ISO, and other styles
More sources

Books on the topic "Drug receptors"

1

Tiligada, Ekaterini, and Madeleine Ennis, eds. Histamine Receptors as Drug Targets. New York, NY: Springer New York, 2017. http://dx.doi.org/10.1007/978-1-4939-6843-5.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Smit, Martine J., Sergio A. Lira, and Rob Leurs, eds. Chemokine Receptors as Drug Targets. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2010. http://dx.doi.org/10.1002/9783527631995.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Xie, Wen, ed. Nuclear Receptors in Drug Metabolism. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2008. http://dx.doi.org/10.1002/9780470409107.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Chemokine receptors as drug targets. Weinheim, Germany: Wiley-VCH, 2011.

Find full text
APA, Harvard, Vancouver, ISO, and other styles
5

1967-, Xie Wen, ed. Nuclear receptors in drug metabolism. Hoboken, NJ: John Wiley & Sons, 2008.

Find full text
APA, Harvard, Vancouver, ISO, and other styles
6

1958-, Doods H. N., and Meel, J. C. A. van 1949-, eds. Receptor data for biological experiments. Chichester: Ellis Horwood, 1991.

Find full text
APA, Harvard, Vancouver, ISO, and other styles
7

Kjell, Fuxe, and Agnati Luigi Francesca, eds. Receptor-receptor interactions: A new intramembrane integrative mechanism : proceedings of an international symposium held at the Wenner-Gren Center, Stockholm, October 9th-11th, 1986. New York: Plenum Press, 1987.

Find full text
APA, Harvard, Vancouver, ISO, and other styles
8

Filizola, Marta, ed. G Protein-Coupled Receptors in Drug Discovery. New York, NY: Springer New York, 2015. http://dx.doi.org/10.1007/978-1-4939-2914-6.

Full text
APA, Harvard, Vancouver, ISO, and other styles
9

Leifert, Wayne R., ed. G Protein-Coupled Receptors in Drug Discovery. Totowa, NJ: Humana Press, 2009. http://dx.doi.org/10.1007/978-1-60327-317-6.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

L, Lundstrom Kenneth, and Chiu Mark L, eds. G protein-coupled receptors in drug discovery. Boca Raton: Taylor & Francis, 2005.

Find full text
APA, Harvard, Vancouver, ISO, and other styles
More sources

Book chapters on the topic "Drug receptors"

1

Rivière, Pierre J. M., and Jean-Louis Junien. "Opioid Receptors." In Drug Development, 203–38. Totowa, NJ: Humana Press, 2000. http://dx.doi.org/10.1007/978-1-59259-202-9_8.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Kumar, T. Durai Ananda. "Receptors." In Drug Design: A Conceptual Overview, 35–58. London: CRC Press, 2022. http://dx.doi.org/10.1201/9781003298755-2.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Schmidhammer, H. "Opioid Receptors." In Drug Addiction and AIDS, 143–48. Vienna: Springer Vienna, 1991. http://dx.doi.org/10.1007/978-3-7091-9173-6_17.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Klebe, Gerhard. "Ligands for Surface Receptors." In Drug Design, 777–812. Berlin, Heidelberg: Springer Berlin Heidelberg, 2013. http://dx.doi.org/10.1007/978-3-642-17907-5_31.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Bain, Gretchen, and T. Jon Seiders. "LPA Receptor Subtypes LPA1and LPA2as Potential Drug Targets." In Lysophospholipid Receptors, 681–708. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2013. http://dx.doi.org/10.1002/9781118531426.ch32.

Full text
APA, Harvard, Vancouver, ISO, and other styles
6

Lewin, Anita H. "Receptors of Mammalian Trace Amines." In Drug Addiction, 327–39. New York, NY: Springer New York, 2008. http://dx.doi.org/10.1007/978-0-387-76678-2_20.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

D’Amato, Massimo, Francesco Makovec, and Lucio C. Rovati. "CCKA Receptors in Gastrointestinal Disorders." In Drug Development, 147–76. Totowa, NJ: Humana Press, 2000. http://dx.doi.org/10.1007/978-1-59259-202-9_6.

Full text
APA, Harvard, Vancouver, ISO, and other styles
8

Youssef, Jihan A., and Mostafa Z. Badr. "PPARs and Drug Metabolism." In Peroxisome Proliferator-Activated Receptors, 71–77. Totowa, NJ: Humana Press, 2013. http://dx.doi.org/10.1007/978-1-62703-420-3_6.

Full text
APA, Harvard, Vancouver, ISO, and other styles
9

Mailman, Richard B., David E. Nichols, and Alexander Tropsha. "Molecular Drug Design and Dopamine Receptors." In The Dopamine Receptors, 105–33. Totowa, NJ: Humana Press, 1997. http://dx.doi.org/10.1007/978-1-4757-2635-0_4.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Gralinski, Michael, Liomar A. A. Neves, and Olga Tiniakova. "Adenosine Receptors." In Drug Discovery and Evaluation: Pharmacological Assays, 1–29. Berlin, Heidelberg: Springer Berlin Heidelberg, 2015. http://dx.doi.org/10.1007/978-3-642-27728-3_140-2.

Full text
APA, Harvard, Vancouver, ISO, and other styles

Conference papers on the topic "Drug receptors"

1

Gabrielli, Ângelo, Camila Sousa Bragunce Alves, Bruna Oliveira Bicalho, and Débora Pimenta Alves. "Benefits and Challenges of Cannabis Use in the Treatment of Refractory Epilepsy." In XIII Congresso Paulista de Neurologia. Zeppelini Editorial e Comunicação, 2021. http://dx.doi.org/10.5327/1516-3180.239.

Full text
Abstract:
Introduction: Refractory epilepsy (RE) is a disease that causes continuous and debilitating seizures. Due to the ineffectiveness of antiepileptic therapies, there is a growing interest in drugs made with cannabidiol (CBD), a substance extracted from Cannabis. Objective: To point out benefits and challenges of the use of CBD in the treatment of RE. Methods: Literature review performed at PubMed, with the descriptors Epilepsy, Drug Therapy and Cannabis. Results: It is suggested that CBD is mediated by cannabinoid receptors coupled to protein G, by blockade of NMDA receptors, by GABAergic modulation, glutamatergic synapses and / or mechanisms involving noncannabinoid receptors. CBD can also oppose the actions of exogenous and endogenous cannabinoid agonists, due to the negative allosteric modulation. The benefits of CBD are: great therapeutic diversity, safety and tolerability, rare and mild side effects, low risk of drug interactions, and milder cognitive effects, when compared to other antiepileptic drugs. Despite the benefits, CBD has adverse effects such as drowsiness, appetite reduction, diarrhea, increased activity of liver enzymes and interaction with substances metabolized by cytochrome P450. Still, the inefficient regulation generates variation in the composition of the marketed drugs, which can lead to Δ9 - tetrahydrocannabinol (THC) intoxication. Conclusions: Thus, it is essential that the scientific community remains open to investigate the effects of CBD, given the advantages of its use for treating RE.
APA, Harvard, Vancouver, ISO, and other styles
2

Pogodaeva, P. S. "Changes in the parameters of a clinical blood test in rats using hypoglycemic agents for the potentiation of drugs with a hepatoprotective effect." In SPbVetScience. FSBEI HE St. Petersburg SUVM, 2023. http://dx.doi.org/10.52419/3006-2023-11-28-34.

Full text
Abstract:
Glucagon-like peptide-1 is an isulin-like peptide hormone from the incretin family. The most popular pharmaceutical analogue of GLP-1 at the moment is liraglutide. GLP-1 receptors are localized in many areas of the brain responsible for the regulation of metabolic processes and eating behavior and in specific areas of the pancreas, heart, blood vessels, immune system, skin and adipose tissue, gastrointestinal tract and kidneys. We can definitely say that the effect of liraglutide extends to all tissues equipped with GLP-1 receptors, while the effect of the drug on the cardiovascular system, immune system, kidneys and gastrointestinal tract is still being studied. Also interesting is the possible effect of liraglutide on the liver, as an organ directly related to lipid and carbohydrate metabolism. In this article, we analyze the possibilities of using Saxenda, the main active ingredient of which is liraglutide, to potentiate the hepatoprotective effects of the Hepaton-vet drug in groups of rats with induced hepatopathy, evaluating the effect of these drugs on the parameters of a clinical blood test.
APA, Harvard, Vancouver, ISO, and other styles
3

Roy, Jyoti, Charity Wayua, and Philip S. Low. "Abstract 2195: Small molecule drug conjugates targeted to cholecystokinin 2 receptors." In Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA. American Association for Cancer Research, 2016. http://dx.doi.org/10.1158/1538-7445.am2016-2195.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Kostić, Marina D., Jovana S. Marjanović, Sven Mangelinckx, and Vera M. Divac. "In silico Drug-Likeness, Pharmacokinetic and other ADME properties of 2- (aminomethyl)cyclopropane-1,1-dicarboxylic acid." In 2nd International Conference on Chemo and Bioinformatics. Institute for Information Technologies, University of Kragujevac, 2023. http://dx.doi.org/10.46793/iccbi23.455k.

Full text
Abstract:
Herein we present the results of in silico determination of Drug-Likeness, Pharmacokinetic and other ADME properties of 2-(aminomethyl)cyclopropane-1,1-dicarboxylic acid as an example constrained γ-amino dicarboxylic acid. The results of in silico screening of drug-likeness, pharmacokinetic and other ADME (absorption, distribution, metabolism and elimination) properties of 2-(aminomethyl)cyclopropane-1,1-dicarboxylic acid have revealed that this compound is not able to cross the blood-brain barrier, but it shows good solubility and gastrointestinal absorption. The possible target screening has indicated the family C G protein-coupled receptors as the most probable physiological targets. More specifically, the 2-(aminomethyl)cyclopropane-1,1-dicarboxylic acid has the highest structural similarity with the known compounds that act on metabotropic glutamate receptor, excitatory amino acid transporter and betaine transporter. Taking all the above into consideration, it can be concluded that our investigated compound could be considered as a candidate molecule for further structural transformations that could enable better pharmacological performance and physiochemical properties.
APA, Harvard, Vancouver, ISO, and other styles
5

"Analogue of glucagon-like peptide-1 - properties, mechanisms of action, prospects for use." In SPbVetScience. FSBEI HE St. Petersburg SUVM, 2023. http://dx.doi.org/10.52419/3006-2023-8-39-44.

Full text
Abstract:
Glucagon-like peptide-1 is an isulin-like peptide hormone from the incretin family. It is secreted by L-cells of the mucous membrane of the ileum and colon, enhances insulin secretion and is a physiological regulator of appetite. The most popular pharmaceutical analogue of GLP-1 at the moment is liraglutide. Liraglutide also activates GLP-1 receptors, but is more stable and allows you to get a more powerful effect due to the prolongation of the drug. It is known that the action of liraglutide extends to all tissues with GLP-1 receptors, but now the drug is used only for correction of body weight and in the complex therapy of patients with type 2 diabetes mellitus. Thus, we have a drug with numerous and multidirectional effects, the full range of possibilities of which has not yet been explored. In this article, we analyze the possibilities of alternative use of this drug, based on literature data.
APA, Harvard, Vancouver, ISO, and other styles
6

PAUWELS, Petrus J. "HUMAN 5-HT1D RECEPTORS: CLONING DISCOVERIES AND THEIR IMPACT ON HUMAN DRUG DESIGN." In IX World Congress of Psychiatry. WORLD SCIENTIFIC, 1994. http://dx.doi.org/10.1142/9789814440912_0026.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Almeida Filho, João L. de, and Jorge H. Fernandez. "HTP SurflexDock: a web tool for Structure-Based Virtual Screening analysis based on the Ensemble Docking protocol." In Brazilian e-Science Workshop. Sociedade Brasileira de Computação - SBC, 2022. http://dx.doi.org/10.5753/bresci.2022.223295.

Full text
Abstract:
Structure-Based Virtual Screening (SVBS) is a technique traditionally used to find a set of specific inhibitors for a receptor structure during the preliminary stages of drug discovery studies. However, more than 90% of SBVS best ranks compounds do not have the expected biological effect at the end of the process. In this context, strategies to increase the success rate must be employed to ensure the experiment's success. Here, we introduce the HTP SurflexDock, a tool that improves the success rate of SBVS experiments through two strategies: First, the ensemble docking protocol enables the simulation of the implicit flexibility of the receptor structure. Second, a post-processing steps allows the user to rescore promising compounds by expanding the conformational space search or estimating the binding free energy through the MM/PBSA protocol. HTP SurflexDock is useful when dealing with flexible receptors and when structural information about the receptor contact area is insufficient or optimized for a specific ligand type. HTP SurflexDock is freely available as a web service or may be downloaded at https://htpsurflexdock.biocomp.uenf.br/.
APA, Harvard, Vancouver, ISO, and other styles
8

Mladenović, Milan P., Nevena M. Tomašević, Sanja Lj Matić, Tamara M. Mladenović, and Rino Ragno. "Computer-aided design of new drugs against breast cancer." In 2nd International Conference on Chemo and Bioinformatics. Institute for Information Technologies, University of Kragujevac, 2023. http://dx.doi.org/10.46793/iccbi23.641m.

Full text
Abstract:
Computational medicinal chemistry, if used properly and in accordance with the available experimental data, may provide significant support to rational drug design. Herein, an overview of the computational approaches that have been applied to an estrogen receptor α (ERα) and endowed in the rational design of pM ERα antagonists with profound anti-breast cancer activity either in vitro or in vivo, will be presented. ERα is a 17β-estradiol inducible transcriptional regulator that initiates the RNA polymerase II-dependent transcriptional machinery, pointed for breast cancer (BC) development via either genomic direct or genomic indirect (i.e., tethered) pathway. To develop innovative ligands, structure-based (SB) 3-D QSAR, ComBinE, and 3-D Pharmacophore studies have been undertaken from experimentally resolved partial agonists, SERMs, and SERDs within either wild-type or mutated ERα receptors. SB and ligand-based (LB) alignments gave rules to align the untested compounds. The protocols led to the development of 3DQs, CBEs, and 3DPQs compounds, further synthesized and submitted to either in vitro or in vivo assessments, upon which new leads were revealed as candidates for clinical trials.
APA, Harvard, Vancouver, ISO, and other styles
9

Богодухова, Екатерина, Ekaterina Bogodukhova, Евгений Байке, and Evgeni Bayke. "GENETIC POLYMORPHISM OF GENES OF TOLL-LIKE RECEPTORS IN VIEW OF DRUG SUSCEPTIBILITY OF MYCOBACTERIUM TUBERCULOSIS." In The VIII Congress of Pulmonologists of Siberia and the Far East with international participation. Far Eastern Scientific Center of Physiology and Pathology of Respiration, 2019. http://dx.doi.org/10.12737/conferencearticle_5ce51ce176bce1.95943239.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Arita, H., and T. Nakano. "INFLUENCE OF β-LACTAM ANTIBIOTICS ON THE PLATELETS IN VITRO EFFECTS OF SOME β-LACTAM ANTIBIOTICS ON THE BIOCHEMICAL RESPONSES OF RAT PLATELETS." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644814.

Full text
Abstract:
The inhibitory mechanism of 3-lactam antibiotics on rat platelets were studied using carbenicil1 in (CBPC) as a representative of the antibiotics. CBPC suppressed all the thrombin-induced cellular responses including shape change, secretion, and aggregation, however, it only suppressed aggregation of ADP-induced responses. This suggests that ADP binding to its own receptor was not affected by the drug while that of thrombin was inhibited. Inhibition of thrombinbinding was confirmed using 125CQSe 0f ADP-stimulated platelets, fibrinogen binding, which has an essential role for ADP-induced primary aggregation, was significantly suppressed by CBPC. Increase of a net negative charge of the membrane surface was observed after treatment of the platelets with antibiotics, and good correlation was obtained between suppression of the platelet responses and degree of net negativecharge of the antibiotics especially on the penicillin analogues. These findings strongly suggest that the inhibition of ligand binding to their own receptors is due to the increase of the negative charge of the platelet membranes which is probably caused by the antibiotic bound to the platelet membrane
APA, Harvard, Vancouver, ISO, and other styles

Reports on the topic "Drug receptors"

1

Harris, Lyndsay N. ERBB-Receptors and Drug Response in Breast Cancer. Fort Belvoir, VA: Defense Technical Information Center, September 1997. http://dx.doi.org/10.21236/adb232291.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Watkins, Linda R., Steven Maier, Ryan Bachtell, Jonathan Katz, and Betty Diamond. Combating Drug Abuse by Targeting Toll-Like Receptor 4 (TLR4). Fort Belvoir, VA: Defense Technical Information Center, October 2013. http://dx.doi.org/10.21236/ada593126.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Xie, Yunhui, and Peng Pang. A Systematic Review and Network Meta-Analysis: Effect of of GLP-1 drugs on weight loss in obese people. INPLASY - International Platform of Registered Systematic Review and Meta-analysis Protocols, June 2022. http://dx.doi.org/10.37766/inplasy2022.6.0074.

Full text
Abstract:
Review question / Objective: 1、Whether GLP-1 drugs have weight loss effect on obese people ? 2、Which GLP-1 drugs are most effective in weight loss among obese people ? Condition being studied: Obesity is an important public health issue that has been on the rise over the last decades. It calls for effective prevention and treatment. Bariatric surgery is the most effective medical therapy for weight loss in morbid obesity, but we are in need for less aggressive treatments. Glucagon-like-peptide-1 receptor agonists are a group of incretin-based drugs that have proven to be productive for obesity treatment. Through activation of the GLP-1 receptor they not only have an important role stimulating insulin secretion after meals, but with their extrapancreatic actions, both peripheral and central, they also help reduce body weight by promoting satiety and delaying gastric emptying.
APA, Harvard, Vancouver, ISO, and other styles
4

Johnson, David A. Spatial Relationships between Drug Binding Sites on the Surface of the Acetylcholine Receptor. Fort Belvoir, VA: Defense Technical Information Center, October 1986. http://dx.doi.org/10.21236/ada222751.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Johnson, David A. Spatial Relationships between Drug Binding Sites on the Surface of the Acetylcholine Receptor. Fort Belvoir, VA: Defense Technical Information Center, February 1989. http://dx.doi.org/10.21236/ada228229.

Full text
APA, Harvard, Vancouver, ISO, and other styles
6

Chen, Yona, Jeffrey Buyer, and Yitzhak Hadar. Microbial Activity in the Rhizosphere in Relation to the Iron Nutrition of Plants. United States Department of Agriculture, October 1993. http://dx.doi.org/10.32747/1993.7613020.bard.

Full text
Abstract:
Iron is the fourth most abundant element in the soil, but since it forms insoluble hydroxides at neutral and basic pH, it often falls short of meeting the basic requirements of plants and microorganisms. Most aerobic and facultative aerobic microorganisms possess a high-affinity Fe transport system in which siderophores are excreted and the consequent Fe complex is taken up via a cognate specific receptor and a transport pathway. The role of the siderophore in Fe uptake by plants and microorganisms was the focus of this study. In this research Rhizopus arrhizus was found to produce a novel siderophore named Rhizoferrin when grown under Fe deficiency. This compound was purified and its chemical structure was elucidated. Fe-Rhizoferrin was found to alleviate Fe deficiency when applied to several plants grown in nutrient solutions. It was concluded that Fe-Rhizoferrin is the most efficient Fe source for plants when compared with other among microbial siderophores known to date and its activity equals that of the most efficient synthetic commercial iron fertilizer-Fe EDDHA. Siderophores produced by several rhizosphere organisms including Rhizopus Pseudomonas were purified. Monoclonal antibodies were produced and used to develop a method for detection of the siderophores produced by plant-growth-promoting microorganisms in barley rhizosphere. The presence of an Fe-ferrichrome uptake in fluorescent Pseudomonas spp. was demonstrated, and its structural requirements were mapped in P. putida with the help of biomimetic ferrichrome analogs. Using competition experiments, it was shown that FOB, Cop B and FC share at least one common determinant in their uptake pathway. Since FC analogs did not affect FOB or Cop-mediated 55Fe uptake, it could be concluded that these siderophores make use of a different receptor(s) than FC. Therefore, recognition of Cop, FOB and FC proceeds through different receptors having different structural requirements. On the other hand, the phytosiderophores mugineic acid (MA and DMA), were utilized indirectly via ligand exchange by P. putida. Receptors from different biological systems seem to differ in their structural requirements for siderophore recognition and uptake. The design of genus- or species-specific drugs, probes or chemicals, along with an understanding of plant-microbe and microbe-microbe relationships as well as developing methods to detect siderophores using monoclonal antibodies are useful for manipulating the composition of the rhizosphere microbial population for better plant growth, Fe-nutrition and protection from diseases.
APA, Harvard, Vancouver, ISO, and other styles
7

Eldefrawi, M. E., and E. X. Albuquerque. Neurotransmitter Receptors and Their Ionic Channels as Targets for Drugs and Toxins. Fort Belvoir, VA: Defense Technical Information Center, January 1985. http://dx.doi.org/10.21236/ada151508.

Full text
APA, Harvard, Vancouver, ISO, and other styles
8

PENNSYLVANIA UNIV PHILADELPHIA. Discovery of Peptidomimetric Antagonists of Estrogen Receptor - Coactivator Interactions: A Novel Strategy to Combat Tamoxifen Drug Resistance. Fort Belvoir, VA: Defense Technical Information Center, October 2001. http://dx.doi.org/10.21236/ada398889.

Full text
APA, Harvard, Vancouver, ISO, and other styles
9

Efange, Simon, and Deborah C. Mash. Drug Development and Conservation of Biodiversity in West and Central Africa: Performance of Neurochemical and Radio Receptor Assays of Plant Extracts Drug Discovery for the Central Nervous System. Fort Belvoir, VA: Defense Technical Information Center, September 2004. http://dx.doi.org/10.21236/ada474867.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Mash, Deborah C. Drug Development and Conservation in West and Central Africa/Performance of Neurochemical and Radio Receptor Assays of Plant Extracts. Fort Belvoir, VA: Defense Technical Information Center, September 2002. http://dx.doi.org/10.21236/ada409688.

Full text
APA, Harvard, Vancouver, ISO, and other styles
You might also be interested in the extended bibliographies on the topic 'Drug receptors' for particular source types:
Journal articles Dissertations / Theses Books
We offer discounts on all premium plans for authors whose works are included in thematic literature selections. Contact us to get a unique promo code!

To the bibliography