RS 102221 (hydrochloride)

RS 102221 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT_2C.¹ It binds to 5-HT_2C receptors (K_i = 3.8 nM for the recombinant human receptor) and is selective for 5-HT_2C receptors over 5-HT_2A and 5-HT_2B receptors (K_is = 1,122.02 and 812.83 nM, respectively), as well as a panel of additional neurotransmitter receptors and ion channels (K_is = ≥316.23 nM for all). RS 102221 inhibits 5-HT-induced increases in the extracellular media acidification rate of CHO-K1 cells expressing human 5-HT_2C receptors (pA₂ = 8.1). It increases food intake and weight gain in rats when administered at a dose of 2 mg/kg. RS 102221 (2 mg/kg) increases the time spent in the light compartment in the light-dark exploration test in mice and reduces prepulse inhibition of the startle reflex when administered at a dose of 1 mg/kg.²

WARNING This product is not for human or veterinary use.

1. Bonhaus, D.W., Weinhardt, K.K., Taylor, M., et al. RS-102221: A novel high affinity and selective, 5-HT_2C receptor antagonist. Neuropharmacology 36(4-5), 621-629 (1997).

2. Kuznetsova, E.G., Amstislavskaya, T.G., Shefer, E.A., et al. Effect of 5-HT_2C receptor antagonist RS 102221 on mouse behavior. Bull. Exp. Biol. Med. 142(1), 76-79 (2006).