SB-243213 (hydrochloride)

SB-243213 is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2C. It is selective for 5-HT2C over 5-HT2A and 5-HT2B receptors (Kis = 0.001, 0.158, and 0.1 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >100, 23, >100, >100, and >100 µM, respectively). SB-243213 reduces the basal activity of 5-HT2C in HEK293 cells expressing the human 5-HT2C receptor (pKB = 9.5). It reverses mCPP-induced hypolocomotion in rats (ID50 = 0.7 mg/kg). SB-243213 (0.2-5 mg/kg) has anxiolytic-like activity in the social interaction test in rats.Formal Name: 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-1H-indole-1-carboxamide, dihydrochloride. CAS Number: 1780372-25-9. Molecular Formula: C22H19F3N4O2 . 2HCl. Formula Weight: 501.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 50mM, Ethanol: 100mM. SMILES: O=C(N1C2=C(CC1)C=C(C)C(C(F)(F)F)=C2)NC3=CN=C(OC4=C(C)N=CC=C4)C=C3.Cl.Cl. InChi Code: InChI=1S/C22H19F3N4O2.2ClH/c1-13-10-15-7-9-29(18(15)11-17(13)22(23,24)25)21(30)28-16-5-6-20(27-12-16)31-19-4-3-8-26-14(19)2,,/h3-6,8,10-12H,7,9H2,1-2H3,(H,28,30),2*1H. InChi Key: UKMTYUXWLKQDNT-UHFFFAOYSA-N.