Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: (1,1-dioxido-4-thiomorpholinyl)[6-[[3-(4-fluorophenyl)-5-methyl-4-isoxazolyl]methoxy]-3-pyridinyl]-methanone
Purity: ≥95%
Formula Markup: C21H20FN3O5S
Formula Weight: 445.5
CAS Number: 1159600-41-5
Notes: Basmisanil is a negative allosteric modulator of α5 subunit-containing GABAA receptors (Ki = 0.005 µM in HEK293 cells expressing the human α5β3γ2 subunit-containing GABAA receptor).{58869} It selectively binds to α5 over α1, α2, or α3 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 α5β3γ2 subunit-containing GABAA receptor (IC50 = 0.008 µM), an effect that can be blocked by flumazenil (Item No. 14252). It reverses diazepam-induced cognitive impairments in rats in the Morris water maze when administered at a dose of 10 mg/kg.
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