Abstract
Zopiclone (ZPC; RP 27, 267) is a new hypnotic which belongs to the new family of cyclopyrrolones chemically unrelated to benzodiazepines (BZD). Psychopharmacological studies on ZPC have shown that it exhibits the five main types of activities —anti-convulsant, anti-agressive, myorelaxant, sedative-hypnotic and anti-conflict (anxiolytic) — which have been considered as being partly those of barbiturates and more specifically those of minor tranquilizers of the BZD type. ZPC possesses in rat brain a high affinity for BZD receptors (Ki values of 36 nM in hippocampus and 22.5 nM in cerebellum). ZPC does not recognize other brain receptors even the peripheral BZD receptor sites. Studies performed with [3H]-ZPC have confirmed the high affinity of ZPC (KD = 13 4 nM in hippocampus). ZPC binding is not enhanced by GABA, or barbiturates and is less sensitive to photoaffinity labelling (low photoshift) than BZD agonists. These results could indicate that ZPC acts on a site distinct from BZD.Centre de Recherches de Vitry, 13, quai Jules Guesde, 94407 Vitry sur Seine, Cedex —France
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