RS 102221 (hydrochloride)

RS 102221 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2C. It binds to 5-HT2C receptors (Ki = 3.8 nM for the recombinant human receptor) and is selective for 5-HT2C receptors over 5-HT2A and 5-HT2B receptors (Kis = 1,122.02 and 812.83 nM, respectively), as well as a panel of additional neurotransmitter receptors and ion channels (Kis = >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-HT2C 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.Formal Name: N-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)-benzenesulfonamide, monohydrochloride. CAS Number: 187397-18-8. Molecular Formula: C27H31F3N4O7S . HCl. Formula Weight: 649.1. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 100 mM. SMILES: O=C(C1=CC(NS(=O)(C2=CC=C(C(F)(F)F)C=C2)=O)=C(C=C1OC)OC)CCCCN3CCC4(NC(NC4=O)=O)CC3.Cl. InChi Code: InChI=1S/C27H31F3N4O7S.ClH/c1-40-22-16-23(41-2)20(33-42(38,39)18-8-6-17(7-9-18)27(28,29)30)15-19(22)21(35)5-3-4-12-34-13-10-26(11-14-34)24(36)31-25(37)32-26,/h6-9,15-16,33H,3-5,10-14H2,1-2H3,(H2,31,32,36,37),1H. InChi Key: SZJZEJZLRDIHPB-UHFFFAOYSA-N.