RS-102221 is a highly potent, selective 5-HT2C receptor antagonist with pKi of 8.4 and 8.5 for human and rat 5-HT2C, respectively.
RS-102221 demonstrates 100-fold selectivity for the 5-HT2C versus 5-HT2A and 5-HT2B receptors.
RS-102221 acts as an antagonist in a cell-based microphysiometry functional assay with pA2 of 8.1 and has no detectable intrinsic efficacy; increases food-intake and weight-gain in rats (2 mg/kg, i.p.).
RS-102221 reverses the inhibitory effects of MK-212 and DOI on 'monosynaptic and 'intermediate' neurones.
