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RS-127445
RS-127445 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x selectivity over the closely related 5-HT2A and 5-HT2C receptors.〔Bonhaus DW, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, Chang LK, Pulido-Rios T, Webber A, Leung E, Eglen RM, Martin GR. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. ''British Journal of Pharmacology''. 1999 Jul;127(5):1075-82. PMID 10455251〕 The role of the 5-HT2B receptor in the body is still poorly understood, and RS-127445 has been a useful tool in unravelling the function of the various systems in which this receptor is expressed.〔Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L. Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension. ''Nature Medicine''. 2002 Oct;8(10):1129-35. PMID 12244304〕〔Kelly CR, Sharif NA. Pharmacological evidence for a functional serotonin-2B receptor in a human uterine smooth muscle cell line. ''Journal of Pharmacology and Experimental Therapeutics''. 2006 Jun;317(3):1254-61. PMID 16517693〕〔Mbaki Y, Ramage AG. Investigation of the role of 5-HT2 receptor subtypes in the control of the bladder and the urethra in the anaesthetized female rat. ''British Journal of Pharmacology''. 2008 Oct;155(3):343-56. PMID 18604238〕
==References==
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