1 The sphingosine 1 - phosphate receptor 2 antagonist , JTE - 013 , 2 increases the excitability of sensory neurons independently of the receptor 3 4 5 Running title :
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7 8 Chao Li, Xian Xuan Chi, Wenrui Xie, J.A. Strong, J-M Zhang, and G.D. Nicol* 9 10 Medical Neuroscience Program, Department of Pharmacology and Toxicology, School of 11 Medicine, Indiana University, Indianapolis, IN, USA 46202; Pain Research Center, Department 12 of Anesthesiology, University of Cincinnati College of Medicine, 231 Albert Sabin Way, PO Box 13 670531, Cincinnati, OH 45267-0531 14 15 16 17 *Corresponding Author: 18 Grant Nicol, Ph.D. 19 Department of Pharmacology and Toxicology 20 635 Barnhill Drive 21 Indiana University School of Medicine 22 Indianapolis, IN USA 46202 23 Office: (317) 274-1570 FAX: (317) 274-7714 Email: [email protected] 24 25 26
منابع مشابه
Sphingosine 1-phosphate receptor 2 antagonist JTE-013 increases the excitability of sensory neurons independently of the receptor.
Previously we demonstrated that sphingosine 1-phosphate receptor 1 (S1PR(1)) played a prominent, but not exclusive, role in enhancing the excitability of small-diameter sensory neurons, suggesting that other S1PRs can modulate neuronal excitability. To examine the potential role of S1PR(2) in regulating neuronal excitability we used the established selective antagonist of S1PR(2), JTE-013. Here...
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Receptors for sphingosine-1-phosphate (S1P) have been identified only recently. Their medicinal chemistry is therefore still in its infancy, and few selective agonists or antagonists are available. Furthermore, the selectivity of S1P receptor agonists or antagonists is not well established. JTE-013 and BML-241 (also known as CAY10444), used extensively as specific S1P(2) and S1P(3) receptors an...
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BACKGROUND AND PURPOSE Sphingosine 1-phosphate (S1P) selectively and potently constricts isolated cerebral arteries, but this response has not been pharmacologically characterized. EXPERIMENTAL APPROACH The receptor subtype(s) involved in S1P-induced cerebrovascular constriction were characterized using genetic (S1P(2) and S1P(3) receptor null mice) and pharmacological tools (phospho-FTY720, ...
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The bioactive lipid sphingosine-1-phosphate (S1P) and its receptors (S1P1-5) play critical roles in many pathologic processes, including cancer. The S1P axis has become a bona fide therapeutic target in cancer. JTE-013 [N-(2,6-dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-hydrazinecarboxamide], a known S1P2 antagonist, suffers from in...
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Sphingosine 1-phosphate (S1P) induces diverse biological responses in various tissues by activating specific G protein-coupled receptors (S1P(1)-S1P(5) receptors). The biological signaling regulated by S1P(3) receptor has not been fully elucidated because of the lack of an S1P(3) receptor-specific antagonist or agonist. We developed a novel S1P(3) receptor antagonist, 1-(4-chlorophenylhydrazono...
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تاریخ انتشار 2012