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Zopiclone

佐匹克隆

Mechanism of action:

Zopiclone 是一種環吡咯酮(cyclopyrrolone)衍生物,是 R+S 外消旋(racemate)混合物。Zopiclone 會與 GABA_A 受體上的 BZ₁ 位點結合,屬於正向變構調節(positive allosteric modulation),增強 GABA 的抑制性作用,增加氯離子通道(Cl⁻ channel)開啟頻率,促使氯離子流入神經元,造成神經元膜電位超極化(hyperpolarization),降低中樞神經興奮性。

​Reference(s):

1. Liu HJ et al. (1985). Pharmacologic studies of the central action of zopiclone: effects on locomotor activity and brain monoamines in rats. Int J Clin Pharmacol Ther Toxicol. 


2. Sato K et al. (1985). Pharmacologic studies of central actions of zopiclone: influence on brain monoamines in rats under stressful condition. Int J Clin Pharmacol Ther Toxicol. 


3. Dundar Y et al. (2004). Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia: a systematic review and meta-analysis. Hum Psychopharmacol.

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