Sedative and anxiolytic effects of
zopiclone's enantiomers and metabolite

Carlson JN, Haskew R, Wacker J,
Maisonneuve IM, Glick SD, Jerussi TP.
Center for Neuropharmacology and Neuroscience,
Albany Medical College,
47 New Scotland Avenue,
12208, Albany, NY, USA
Eur J Pharmacol 2001 Mar 16; 415(2-3):181-9


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 anxiolyic 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.
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