RS-127445 explained

RS-127445 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT_2B receptor, with around 1000 times selectivity over the closely related 5-HT_2A and 5-HT_2C receptors.^[1] The role of the 5-HT_2B 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.^{[2] [3] [4]}

Notes and References

1. 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 . 6 . RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist . British Journal of Pharmacology . 127 . 5 . 1075–82 . July 1999 . 10455251 . 10.1038/sj.bjp.0702632 . 1566110 .
2. Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L . 6 . Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension . Nature Medicine . 8 . 10 . 1129–35 . October 2002 . 12244304 . 10.1038/nm764 . 20736218 .
3. Kelly CR, Sharif NA . Pharmacological evidence for a functional serotonin-2B receptor in a human uterine smooth muscle cell line . The Journal of Pharmacology and Experimental Therapeutics . 317 . 3 . 1254–61 . June 2006 . 16517693 . 10.1124/jpet.105.100172 . 6604193 .
4. 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 . 155 . 3 . 343–56 . October 2008 . 18604238 . 10.1038/bjp.2008.273 . 2567885 .