Sedative and anxiolytic effects of zopiclone's enantiomers and metabolite.

Article Details

Citation

Copy to clipboard

Carlson JN, Haskew R, Wacker J, Maisonneuve IM, Glick SD, Jerussi TP

Sedative and anxiolytic effects of zopiclone's enantiomers and metabolite.

Eur J Pharmacol. 2001 Mar;415(2-3):181-9. doi: 10.1016/s0014-2999(01)00851-2.

PubMed ID

11274997 [ View in PubMed

]

Abstract

We evaluated racemic zopiclone, its (S)- and (R)-enantiomers and a metabolite, (S)-desmethylzopiclone, for their actions on locomotor activity, rotarod performance, the elevated plus maze and the Vogel conflict test of anxiety, and electroconvulsive shock-induced seizures duration. Zopiclone and its (R)- and (S)-enantiomers reduced locomotor activity, and zopiclone and its (S)-enantiomer disrupted rotarod performance at 10 mg/kg. (S)-desmethylzopiclone did not alter these measures at doses of less than 200 mg/kg. (S)-desmethylzopiclone altered plus maze performance at the lowest dose of all the zopiclone derivatives tested, caused a dose-related effect on the Vogel conflict test and caused a dose-related reduction of electroconvulsive shock-induced seizure durations. The data indicate that (S)-desmethylzopiclone can bring about an anxiolytic effect without a substantial degree of central nervous system depression, and suggest that the agent may be particularly useful clinically in the treatment of anxiety.

DrugBank Data that Cites this Article

Drugs

Eszopiclone

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Eszopiclone	Cytochrome P450 3A4	Protein	Humans	Unknown	Substrate	Details