Relevant bibliographies by topics / S1P receptor antagonists

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Academic literature on the topic 'S1P receptor antagonists'

Author: Grafiati
Published: 14 March 2023
Last updated: 31 July 2025

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Journal articles on the topic "S1P receptor antagonists"

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Sumida, Grant M., and W. Daniel Stamer. "S1P2 receptor regulation of sphingosine-1-phosphate effects on conventional outflow physiology." American Journal of Physiology-Cell Physiology 300, no. 5 (2011): C1164—C1171. http://dx.doi.org/10.1152/ajpcell.00437.2010.

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Elevated intraocular pressure is the main risk factor in primary open-angle glaucoma, involving an increased resistance to aqueous humor outflow in the juxtacanalicular region of the conventional outflow pathway which includes the trabecular meshwork (TM) and the inner wall of Schlemm's canal (SC). Previously, sphingosine-1-phosphate (S1P) was shown to decrease outflow facility in porcine and human eyes, thus increasing outflow resistance and intraocular pressure. Owing to S1P's known effect of increasing barrier function in endothelial cells and the robust expression of the S1P1 receptor on t
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Zhang, Dong Dong, Bona Linke, Jing Suo, et al. "Antinociceptive effects of FTY720 during trauma-induced neuropathic pain are mediated by spinal S1P receptors." Biological Chemistry 396, no. 6-7 (2015): 783–94. http://dx.doi.org/10.1515/hsz-2014-0276.

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Abstract FTY720 (fingolimod) is, after its phosphorylation by sphingosine kinase (SPHK) 2, a potent, non-selective sphingosine-1-phosphate (S1P) receptor agonist. FTY720 has been shown to reduce the nociceptive behavior in the paclitaxel model for chemotherapy-induced neuropathic pain through downregulation of S1P receptor 1 (S1P1) in microglia of the spinal cord. Here, we investigated the mechanisms underlying the antinociceptive effects of FTY720 in a model for trauma-induced neuropathic pain. We found that intrathecal administration of phosphorylated FTY720 (FTY720-P) decreased trauma-induc
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Lukas, Susan, Lori Patnaude, Sokol Haxhinasto, et al. "No Differences Observed among Multiple Clinical S1P1 Receptor Agonists (Functional Antagonists) in S1P1 Receptor Down-regulation and Degradation." Journal of Biomolecular Screening 19, no. 3 (2013): 407–16. http://dx.doi.org/10.1177/1087057113502234.

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Sphingosine-1-phosphate (S1P) is a bioactive metabolite with pleiotropic effects on multiple cellular processes in health and disease. Responses elicited by S1P are a result of binding to five specific G-protein–coupled receptors. We have developed multiple assays to systematically study the downstream signaling of these receptors, including early events such as direct receptor activation (GTPγS) as well as more distal events such as S1P1 receptor degradation. Employing such assays, we have characterized and compared multiple S1P1 agonists that are in clinical development including FTY720, BAF
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Hafizi, Redona, Faik Imeri, Roland H. Wenger та Andrea Huwiler. "S1P Stimulates Erythropoietin Production in Mouse Renal Interstitial Fibroblasts by S1P1 and S1P3 Receptor Activation and HIF-2α Stabilization". International Journal of Molecular Sciences 22, № 17 (2021): 9467. http://dx.doi.org/10.3390/ijms22179467.

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Erythropoietin (Epo) is the critical hormone for erythropoiesis. In adults, Epo is mainly produced by a subset of interstitial fibroblasts in the kidney, with minor amounts being produced in the liver and the brain. In this study, we used the immortalized renal interstitial fibroblast cell line FAIK F3-5 to investigate the ability of the bioactive sphingolipid sphingosine 1-phosphate (S1P) to stimulate Epo production and to reveal the mechanism involved. Stimulation of cells with exogenous S1P under normoxic conditions (21% O2) led to a dose-dependent increase in Epo mRNA and protein levels an
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Zhang, Gengqian, Sulei Xu, Yan Qian, and Pingnian He. "Sphingosine-1-phosphate prevents permeability increases via activation of endothelial sphingosine-1-phosphate receptor 1 in rat venules." American Journal of Physiology-Heart and Circulatory Physiology 299, no. 5 (2010): H1494—H1504. http://dx.doi.org/10.1152/ajpheart.00462.2010.

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Sphingosine-1-phosphate (S1P) has been demonstrated to enhance endothelial barrier function in vivo and in vitro. However, different S1P receptor subtypes have been indicated to play different or even opposing roles in the regulation of vascular barrier function. This study aims to differentiate the roles of endogenous endothelial S1P subtype receptors in the regulation of permeability in intact microvessels using specific receptor agonist and antagonists. Microvessel permeability was measured with hydraulic conductivity ( Lp) in individually perfused rat mesenteric venules. S1P-mediated chang
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Werth, Stephan, Helge Müller-Fielitz, and Walter Raasch. "Obesity-stimulated aldosterone release is not related to an S1P-dependent mechanism." Journal of Endocrinology 235, no. 3 (2017): 251–65. http://dx.doi.org/10.1530/joe-16-0550.

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Aldosterone has been identified as an important factor in obesity-associated hypertension. Here, we investigated whether sphingosine-1-phosphate (S1P), which has previously been linked to obesity, increases aldosterone release. S1P-induced aldosterone release was determined in NCI H295R cells in the presence of S1P receptor (S1PR) antagonists. In vivo release of S1P (100–300 µg/kgbw) was investigated in pithed, lean Sprague Dawley (SD) rats, diet-obese spontaneous hypertensive rats (SHRs), as well as in lean or obese Zucker rats. Aldosterone secretion was increased in NCI H295R cells by S1P, t
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Corvino, Angela, Ida Cerqua, Alessandra Lo Bianco, et al. "Antagonizing S1P3 Receptor with Cell-Penetrating Pepducins in Skeletal Muscle Fibrosis." International Journal of Molecular Sciences 22, no. 16 (2021): 8861. http://dx.doi.org/10.3390/ijms22168861.

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S1P is the final product of sphingolipid metabolism, which interacts with five widely expressed GPCRs (S1P1-5). Increasing numbers of studies have indicated the importance of S1P3 in various pathophysiological processes. Recently, we have identified a pepducin (compound KRX-725-II) acting as an S1P3 receptor antagonist. Here, aiming to optimize the activity and selectivity profile of the described compound, we have synthesized a series of derivatives in which Tyr, in position 4, has been substituted with several natural aromatic and unnatural aromatic and non-aromatic amino acids. All the comp
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Toebbe, JT, and Mary Beth Genter. "An Update on Sphingosine-1-Phosphate and Lysophosphatidic Acid Receptor Transcripts in Rodent Olfactory Mucosa." International Journal of Molecular Sciences 23, no. 8 (2022): 4343. http://dx.doi.org/10.3390/ijms23084343.

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Olfactory neurons connect the external environment and the brain, allowing the translocation of materials from the nasal cavity into the brain. The olfactory system is involved in SARS-CoV-2 infections; early in the pandemic declared in 2020, a loss of the sense of smell was found in many infected patients. Attention has also been focused on the role that the olfactory epithelium appears to play in the entry of the SARS-CoV-2 virus into the brain. Specifically, SARS-CoV-2 enters cells via the angiotensin-converting enzyme 2 protein (ACE2), which is found on supporting cells in the olfactory ep
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Godessart, Nuria, Sanam Mustafa, Vlad Dolgachev, et al. "The S1P1 receptor antagonist W146 induces lymphopenia in mice. Demonstration that functional antagonism of S1P1 is the mechanism of lymphopenia evoked by fingolimod-like compounds. (140.15)." Journal of Immunology 184, no. 1_Supplement (2010): 140.15. http://dx.doi.org/10.4049/jimmunol.184.supp.140.15.

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Abstract Agonists of sphingosine 1-phosphate receptor 1 (S1P1) are a novel class of immunosuppressants. S1P is the endogenous agonist of S1P1 and promotes lymphocyte egress from lymph nodes (LN) into blood. However, synthetic agonists like fingolimod prevent the egress, causing systemic lymphopenia. This apparent contradiction is explained by the concept of functional antagonism, according to which synthetic S1P1 agonists induce receptor internalization, making cells unresponsive to the endogenous S1P. If this mechanism is true, S1P1 antagonists should induce lymphopenia. We have fully charact
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Juarez, Julius G., Nadia Harun, Marilyn Thien, et al. "Sphingosine-1-phosphate facilitates trafficking of hematopoietic stem cells and their mobilization by CXCR4 antagonists in mice." Blood 119, no. 3 (2012): 707–16. http://dx.doi.org/10.1182/blood-2011-04-348904.

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Abstract CXCL12 and VCAM1 retain hematopoietic stem cells (HSCs) in the BM, but the factors mediating HSC egress from the BM to the blood are not known. The sphingosine-1-phosphate receptor 1 (S1P1) is expressed on HSCs, and S1P facilitates the egress of committed hematopoietic progenitors from the BM into the blood. In the present study, we show that both the S1P gradient between the BM and the blood and the expression of S1P1 are essential for optimal HSC mobilization by CXCR4 antagonists, including AMD3100, and for the trafficking of HSCs during steady-state hematopoiesis. We also demonstra
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Dissertations / Theses on the topic "S1P receptor antagonists"

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Puliti, Elisa. "Role of sphingosine 1-phosphate metabolism and signalling in skeletal muscle atrophy and fibrosis." Doctoral thesis, Università di Siena, 2022. http://hdl.handle.net/11365/1195603.

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In the last 30 years, multiple roles of S1P have been demonstrated in the regulation of skeletal muscle biology. The presented study is focused on the role of S1P metabolism in myogenic differentiation, where SPL was found playing a crucial role in regulating S1P cellular levels and responsible for onset of myogenic program. The role of S1P axis was also confirmed in skeletal muscle atrophy induced by TNF-alpha. S1P signalling pathwayplays a crucial role in the development and maintenance of the fibrotic process. New S1P3 antagonists were tested to antagonise the receptor involved in fibrosis,
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Collier, Lauren Michele. "Relationship Between CB1 and S1P Receptors in the Central Nervous System." VCU Scholars Compass, 2006. http://scholarscompass.vcu.edu/etd/733.

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There is significant sequence homology and anatomical co-distribution between cannabinoid (CB1) and sphingosine-1-phosphate (S1P) receptors in the CNS, but potential functional relationships between these lysolipid receptors have not been examined. Therefore, to investigate possible relationships between these two systems at the level of G-protein activation, agonist-stimulated [35S]GTPγS binding and autoradiography were conducted. Autoradiographic studies were first performed to localize receptor-mediated G-protein activation in mouse brain. Coronal brain slices were processed for stimulation
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Janse, van Rensburg Hendrika Nicolien. "A longitudinal study of the usage of acid reducing medicine using a medicine claims database / Hendrika Nicolien Janse van Rensburg." Thesis, North-West University, 2007. http://hdl.handle.net/10394/1903.

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Acid-related disorders are common, chronic conditions that have considerable impact on a patient's quality of life. In a study conducted by Majumdar et al. (2003:2411) the prevalence of chronic acid-related disorders was 2.3%. Acid-related disorders represent a major financial consideration with respect to the costs of drug prescribing (Whitaker, 1998:6). Health care cost increases each year. This leads to an increased interest in economic evaluation of health care and medical technologies (Anell & Svarvar, 2000:175). Health care providers no longer make treatment decisions independent of the
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Zhu, Ran. "Synthesis and biological evaluation of conformationally constrained sphingosine-1-phosphate analogs as subtype selective S1P receptor agonist/antagonist /." 2008. http://wwwlib.umi.com/dissertations/fullcit/3294775.

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Clemens, Jeremy Justin. "Synthesis of subtype-selective sphingosine-1-phosphate (SIP) receptor agonists and antagonists : elucidation of a structure-activity relationship for SIP and the mechanism of action of FTY720 /." 2004. http://wwwlib.umi.com/dissertations/fullcit/3144658.

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Van, Rensburg Hendrika Nicolien Janse. "A longitudinal study of the usage of acid reducing medicine using a medicine claims database / H.N. Janse van Rensburg." Thesis, 2007. http://hdl.handle.net/10394/1903.

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Books on the topic "S1P receptor antagonists"

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Alhazzani, Waleed, and Deborah J. Cook. Stress ulcer prophylaxis and treatment drugs in critical illness. Oxford University Press, 2016. http://dx.doi.org/10.1093/med/9780199600830.003.0041.

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Many changes have occurred over the last three decades in the field of stress ulcer gastrointestinal bleeding and its prevention. The topic is controversial, fuelled by disparate data, studies at risk of bias, and the impression that the problem is not as serious as it once was. Indeed, compared with over four decades ago when mucosal ulceration of the stomach causing serious bleeding was first described, a relatively small proportion of critically-ill patients now develop clinically important bleeding. Acid suppression is commonly prescribed for stress ulcer prophylaxis (SUP), targeting subgr
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Book chapters on the topic "S1P receptor antagonists"

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Bergeron, R., C. de Montigny, and P. Blier. "Potentiation of the Antidepressant Effect of Selected Drugs by the Antagonism of Presynaptic 5-HT1AReceptors." In New Therapeutic Indications of Antidepressants. KARGER, 1997. http://dx.doi.org/10.1159/000061356.

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Shah, Manoj. "Intervention of PAR-2 Mediated CGRP in Animal Model of Visceral Hyperalgesia." In Animal Models and Experimental Research in Medicine [Working Title]. IntechOpen, 2023. http://dx.doi.org/10.5772/intechopen.106859.

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Protease-activated receptor-2 (PAR-2) mediates calcitonin gene-related peptide (CGRP) release and collectively plays a crucial role in inflammation-induced visceral hyperalgesia (VH). The present review chapter outlines the substantial advances that elucidated the underlying role of PAR-2 and CGRP in gut inflammation-induced VH and highlights their relevancies in the management of VH. PAR-2 is expressed in a wide range of gastrointestinal cells and its activation on primary afferent nerves by tryptase, trypsin or cathepsin-S is the key mechanism of sensitization during intestinal inflammation.
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Theard, M. Angele, and Alexandra Bastien. "Intraoperative Hyperkalemia." In Anesthesiology: A Problem-Based Learning Approach, edited by Tracey Straker and Shobana Rajan. Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780190850692.003.0031.

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Patients with hypertension, diabetes, and heart disease are at risk for chronic kidney disease and therefore require close monitoring of potassium (K<sup>+</sup>) levels in order to avoid some of the more concerning consequences of hyperkalemia. Medical therapy in these patients, which often includes angiotensin converting enzyme inhibitors, angiotensin receptor blockers, renin inhibitors, and mineralocorticoid receptor antagonists, while helpful in managing some of the aforementioned comorbidities and ameliorating chronic kidney disease in these patients, places them at increased risk for unw
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Hill, D. R., L. Singh, P. Boden, R. Pinnock, G. N. Woodruff,, and J. Hughes. "Detection of CCK receptor subtypes in mammalian brain using highly selective non-peptide antagonists." In Multiple Cholecystokinin Receptors in the CNS. Oxford University PressOxford, 1992. http://dx.doi.org/10.1093/oso/9780198577560.003.0005.

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Abstract The neuropeptide CCK occurs in the mammalian CNS in a variety of molecular forms, but it is the sulphated octapeptide (CCK-8S) that predominates (Vanderhaeghen et al. 1975; Dockray 1976; Rehfeld 1978; Larsson and Rehfeld 1979). Since its discovery in brain, the effects of CCK-8S and of related peptide fragments such as CCK-4 and pentagastrin have been studied extensively in a wide variety of systems. These studies have led to the implication of CCK in a variety of physiological systems. For instance, CCK has been suggested as an endogenous satiety factor and as such may play an import
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Conference papers on the topic "S1P receptor antagonists"

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Vanhoutte, Paul M. "PLATELETS, ENDOTHELIUM AND VASOSPASM." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643722.

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The endothelium can secrete both relaxing and contracting substances. One of the most powerful stimuli to the release of the former are thrombin and aggregating platelets. This contributes to the protective role of the endothelium against inappropriate intraluminal platelet aggregation and coagulation in blood vessels with an intact intima. Thrombin-induced, endothelium-dependent relaxations have been obtained in isolated arteries of different species, including humans. Endothelium-dependent relaxations can be evoked by autologous platelets in isolated blood vessels of the dog, pig and rat; th
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Mansfield, B., P. Huang, R. Bruce, et al. "T4 Calcium-sensing receptor antagonists (calcilytics) as a novel therapeutic for alarmin-driven inflammatory lung disease." In British Thoracic Society Winter Meeting 2019, QEII Centre, Broad Sanctuary, Westminster, London SW1P 3EE, 4 to 6 December 2019, Programme and Abstracts. BMJ Publishing Group Ltd and British Thoracic Society, 2019. http://dx.doi.org/10.1136/thorax-2019-btsabstracts2019.4.

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Simin, Faria Anjum, and Joseph Schober. "Subcellular Localization Analysis of Sigma 1 Receptor (S1R) and Binding Immunoglobulin Protein (BiP) for Identification of Antagonists versus Agonists." In ASPET 2023 Annual Meeting Abstracts. American Society for Pharmacology and Experimental Therapeutics, 2023. http://dx.doi.org/10.1124/jpet.122.176040.

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Birring, SS, L. Cardozo, P. Dicpinigaitis, et al. "S1 A phase 3b trial of gefapixant, a P2X3-receptor antagonist, in women with chronic cough and stress urinary incontinence." In British Thoracic Society Winter Meeting 2023, QEII Centre, Broad Sanctuary, Westminster, London SW1P 3EE, 22 to 24 November 2023, Programme and Abstracts. BMJ Publishing Group Ltd and British Thoracic Society, 2023. http://dx.doi.org/10.1136/thorax-2023-btsabstracts.7.

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Birring, SS, LP McGarvey, JA Smith, et al. "S28 Benefits observed with patient-reported outcomes in a phase 2b clinical trial of gefapixant, a P2X3 receptor antagonist, in chronic cough." In British Thoracic Society Winter Meeting 2019, QEII Centre, Broad Sanctuary, Westminster, London SW1P 3EE, 4 to 6 December 2019, Programme and Abstracts. BMJ Publishing Group Ltd and British Thoracic Society, 2019. http://dx.doi.org/10.1136/thorax-2019-btsabstracts2019.34.

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Bailo, M., L. Dunning, J. Brzeszczynska, et al. "S100 Reduction of inflammatory cytokine production in chronic obstructive pulmonary disease (COPD) epithelial cells by protease activated receptor 2 (PAR2) antagonism." In British Thoracic Society Winter Meeting 2019, QEII Centre, Broad Sanctuary, Westminster, London SW1P 3EE, 4 to 6 December 2019, Programme and Abstracts. BMJ Publishing Group Ltd and British Thoracic Society, 2019. http://dx.doi.org/10.1136/thorax-2019-btsabstracts2019.106.

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Reports on the topic "S1P receptor antagonists"

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Rafaeli, Ada, Russell Jurenka, and Chris Sander. Molecular characterisation of PBAN-receptors: a basis for the development and screening of antagonists against Pheromone biosynthesis in moth pest species. United States Department of Agriculture, 2008. http://dx.doi.org/10.32747/2008.7695862.bard.

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The original objectives of the approved proposal included: (a) The determination of species- and tissue-specificity of the PBAN-R; (b) the elucidation of the role of juvenile hormone in gene regulation of the PBAN-R; (c) the identificationof the ligand binding domains in the PBAN-R and (d) the development of efficient screening assays in order to screen potential antagonists that will block the PBAN-R. Background to the topic: Moths constitute one of the major groups of pest insects in agriculture and their reproductive behavior is dependent on chemical communication. Sex-pheromone blends are
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