SB-742457

SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM). SB-742457 (1 µM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity. SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells. In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine (Cay-14108) in rats. It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management.Formal Name: 3-(phenylsulfonyl)-8-(1-piperazinyl)-quinoline. CAS Number: 607742-69-8. Synonyms: GSK742457. Molecular Formula: C19H19N3O2S. Formula Weight: 353.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, Ethanol: 0.1 mg/ml. lambdamax: 273, 364 nm. SMILES: O=S(C(C=N1)=CC2=C1C(N3CCNCC3)=CC=C2)(C4=CC=CC=C4)=O. InChi Code: InChI=1S/C19H19N3O2S/c23-25(24,16-6-2-1-3-7-16)17-13-15-5-4-8-18(19(15)21-14-17)22-11-9-20-10-12-22/h1-8,13-14,20H,9-12H2. InChi Key: JJZFWROHYSMCMU-UHFFFAOYSA-N.