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Estazolam

艾司唑侖

Mechanism of action:

Estazolam 是一種 1,4-苯二氮平（1,4-benzodiazepine）衍生物。Estazolam 能結合 GABA_A 受體的苯二氮平結合位點（benzodiazepine-binding site），提高 GABA 與其受體的親和力，使氯離子通道（Cl⁻ channel）開啟頻率增加，導致氯離子流入神經元，造成細胞膜超極化（hyperpolarization），與鎮靜、催眠、抗焦慮及抗痙攣等中樞抑制相關效應有關。

​Reference(s):

1. Watanabe S et al. (1986). Electroencephalographic effects of 450191-S and its metabolites in rabbits with chronic electrode implants. Nihon Yakurigaku Zasshi. 


2. Oishi R et al. (1986). Diazepam-induced decrease in histamine turnover in mouse brain. Eur J Pharmacol. 


3. Usami N et al. (2002). Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull.

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