Basmisanil

Basmisanil is a negative allosteric modulator of alpha5 subunit-containing GABAA receptors (Ki = 0.005 µM in HEK293 cells expressing the human alpha5beta3gamma2 subunit-containing GABAA receptor). It selectively binds to alpha5 over alpha1, alpha2, or alpha3 subunit-containing GABAA receptors (Kis = 1.031, 0.458, and 0.51 µM, respectively) as well as a panel of 78 receptors, transporters, and ion channels at 10 µM. Basmisanil inhibits GABA-induced currents in Xenopus oocytes expressing the human alpha5beta3gamma2 subunit-containing GABAA receptor (IC50 = 0.008 µM), an effect that can be blocked by flumazenil (Cay-14252). It reverses diazepam-induced cognitive impairments in rats in the Morris water maze when administered at a dose of 10 mg/kg.Formal Name: (1,1-dioxido-4-thiomorpholinyl)[6-[[3-(4-fluorophenyl)-5-methyl-4-isoxazolyl]methoxy]-3-pyridinyl]-methanone. CAS Number: 1159600-41-5. Synonyms: RG-1662. Molecular Formula: C21H20FN3O5S. Formula Weight: 445.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml. lambdamax: 233 nm. SMILES: O=S1(CCN(C(C2=CC=C(OCC3=C(C)ON=C3C4=CC=C(F)C=C4)N=C2)=O)CC1)=O. InChi Code: InChI=1S/C21H20FN3O5S/c1-14-18(20(24-30-14)15-2-5-17(22)6-3-15)13-29-19-7-4-16(12-23-19)21(26)25-8-10-31(27,28)11-9-25/h2-7,12H,8-11,13H2,1H3. InChi Key: VCGRFBXVSFAGGA-UHFFFAOYSA-N.