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Eszopiclone

艾司佐匹克隆
Mechanism of action:
Eszopiclone 是佐匹克隆(zopiclone)的 S-對映異構物(S-enantiomer)。Eszopiclone 會與 GABA_A 受體上的苯二氮平結合位點(對含 α1 亞基受體有較高親和性)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. Greenblatt DJ et al. (2012). Pharmacokinetic evaluation of eszopiclone: clinical and therapeutic implications. Expert Opin Drug Metab Toxicol.
2. Carlson JN et al. (2001). Sedative and anxiolytic effects of zopiclone's enantiomers and metabolite. Eur J Pharmacol.
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