Potent and selective 5-HT2C antagonist (pKi = 8.7). Displays ~ 100-fold selectivity over the 5-HT2A and 5-HT2B subtypes and is > 100-fold selective over other 5-HT receptors, α- and β-adrenergic and muscarinic ACh receptors.
Bonhaus et al (1997) RS-102221: a novel high affinity and selective 5-HT2C receptor antagonist. Neuropharmacology 36 621 PMID:9225287 |Bonhaus et al (1998) Absorption and brain penetration of a high affinity, highly selective 5-HT2C receptor antagonist, RS-102221. Ann.N.Y.Acad.Sci. 861 269 PMID:9928284 |Weinhardt et al (1996) Some benzenesulphonamido-substituted valerophenones that are selective antagonists for the 5-HT2C receptor. Bioorg.Med.Chem.Lett. 6 2687