Basmisanil (RG1662) 是一种高选择性含 α 亚基 GABAA 受体 (GABAAα5) 的负变构调节剂，具有口服活性。Basmisanil 可以抑制 GABAA-α5， K_i 值为 5 nM 和 IC₅₀ 值为 8 nM。Basmisanil 可用于多种认知和精神障碍的研究。

Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a K i value of 5 nM and IC 50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.

Solid

IC50: 8 nM (GABAAα5)
Ki: 5 nM (GABAAα5); 1031 nM (GABAAα1); 458 nM (GABAAα2); 510 nM (GABAAα3)

Basmisanil (0.1 nM-100 μM) has high affinity for bounding to recombinant human GABAA-α5 receptors with a Ki value of 5 nM and more than 90-fold selectivity versus α1 (Ki = 1031 nM), α2 (Ki = 458 nM), and α3 (Ki = 510 nM) subunit-containing receptors.
Basmisanil (1 nM-1 μM) shows a highly selective inhibition of GABAA-α5 with a IC50 value of 8 nM.
Basmisanil (1 μM) inhibits GABA-induced currents at GABAA-α5 yet had little or no effect at the other receptor subtypes. has not independently confirmed the accuracy of these methods. They are for reference only.

Basmisanil (3-100 mg/kg, p.o.) occupies GABAA-α receptor in dose-dependent in rat brain.
Basmisanil (3-600 mg/kg p.o.) improves cognition in rats and non.human primates and not show anxiogenic or proconvulsant effects.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Joerg F Hipp, et al. Basmisanil, a highly selective GABA A-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man. Sci Rep. 2021 Apr 8;11(1):7700.

In Vitro: DMSO : 100 mg/mL (224.49 mM; Need ultrasonic)配制储备液