The mechanism of action of zopiclone.

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Doble A, Canton T, Malgouris C, Stutzmann J, Piot O, Bardone M, Pauchet C, Blanchard J

The mechanism of action of zopiclone.

Eur Psychiatry. 1995;10 Suppl 3:117s-28s. doi: 10.1016/0924-9338(96)80093-9.

PubMed ID

19698408 [ View in PubMed

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Abstract

The mechanism of action of the cyclopyrrolone hypnotic drug zopiclone involves allosteric modulation of the GABAA receptor. Zopiclone displaces the binding of [(3)H]-flunitrazepam with an affinity of 28 nM, and enhances the binding of the channel blocker [(35)S]-TBPS. The binding of zopiclone, unlike that of hypnotic benzodiazepines, is not facilitated by GABA. Zopiclone does not distinguish between GABAA receptors containing different alpha-subunits (BZ(1) and BZ(2) phenotype). Studies with protein-modifying agents (eg diethylpyrocarbonate) and photoaffinity labelling suggest that cyclopyrrolones bind to a domain on the GABAA receptor different from the benzodiazepine binding domain. The consequence of this interaction with the GABAA receptor is to potentiate responses to GABA, as can be demonstrated by electrophysiological methods. Subchronic treatment of mice with high doses of zopiclone does not produce the changes in sensitivity of the GABAA receptor that are observed with hypnotic benzodiazepines.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Eszopiclone	GABA(A) Receptor (Protein Group)	Protein group	Humans	Yes	Positive allosteric modulator	Details