Alpidem 选择性地与含有 α1β2γ2 亚基的 GABAA 受体结合，IC50 为 17 nM，并发挥抗焦虑作用。
货号:ajcx25370
CAS:82626-01-5
分子式:C21H23Cl2N3O
分子量：404.3
溶解度:Chloroform: slightly soluble,Methanol: slightly soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Alpidem is an anxiolytic agent.¹It selectively binds to α₁β₂γ₂subunit-containing GABA_Areceptors over α₅β₂γ₂subunit-containing GABA_Areceptors in HEK293 cells (IC₅₀s = 0.017 and ≥10 µM, respectively, for the recombinant rat receptors).²Alpidem also binds to the GABA_A/benzodiazepine receptor complex and translocator protein 18 kDa (TSPO) with IC₅₀values of 0.028 and 0.0079 µM, respectively.³It reduces marble burying in mice, indicating anxiolytic activity, with a minimum effective dose (MED) of 10 mg/kg.⁴Unlike the benzodiazepine alprazolam, alpidem does not induce sedation in mice when administered at doses up to 2 mg/kg.⁵Formulations containing alpidem have previously been used in the treatment of generalized anxiety disorder.

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