Basmisanil

Basmisanil is a negative allosteric modulator of α₅ subunit-containing GABA_A receptors (K_i = 0.005 µM in HEK293 cells expressing the human α₅β₃γ₂ subunit-containing GABA_A receptor).¹ It selectively binds to α₅ over α₁, α₂, or α₃ subunit-containing GABA_A receptors (K_is = 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 GABA_A 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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1. Hipp, J.F., Knoflach, F., Comley, R., et al. Basmisanil, a highly selective GABA_A-α5 negative allosteric modulator: Preclinical pharmacology and demonstration of functional target engagement in man. Sci. Rep. 11(1), 7700 (2021).