Zopiclone

Mechanism of action:
Zopiclone is a cyclopyrrolone derivative and a racemic mixture of the R and S enantiomers. It binds to the BZ₁ site on the GABA_A receptor and acts as a positive allosteric modulator. By enhancing the inhibitory action of GABA, it increases the frequency of chloride channel opening, promotes chloride influx into neurons, induces membrane hyperpolarization, and reduces central nervous system excitability.
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.
