Catalog No.: PC-27111Not For Human Use, Lab Use Only.
RS-127445 hydrochloride is a potent, selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with pKi of 9.5, 1,000 fold selectivity over numerous other receptor and ion channel binding sites.
RS-127445 hydrochloride is a potent, selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with pKi of 9.5, 1,000 fold selectivity over numerous other receptor and ion channel binding sites. RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1) in cells expressing human recombinant 5-HT2B receptors. RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3). RS-127445 (5 mg/kg, i.p.) produced plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4 h.
