Description and references

Cyclopyrrolone member of a family of non-benzodiazepine GABA_A receptor agonists. Prepn: C. Cotrel et al., DE 2300491; eidem, US 3862149 (1973, 1975 both to Rhone-Poulenc); C. Jeanmart, C. Cotrel, C. R. Seances Acad. Sci. Ser. C 287, 377 (1978). In vitro and in vivo inhibition of benzodiazepine binding: J. C. Blanchard et al., Life Sci. 24, 2417 (1979); see also P. H. Wu et al., ibid. 28, 1023 (1981). Comparative study with benzodiazepines: E. Wickstrm, K. E. Giercksky, Eur. J. Clin. Pharmacol. 17, 93 (1980). HPLC determn of enantiomers in plasma: C. Fernandez et al., J. Chromatogr.572, 195 (1991); in urine: eidem, ibid. 617, 271 (1993). Pharmacokinetics of zopiclone and enantiomers: eidem, Drug Metab. Dispos. 21, 1125 (1993). Mechanism of action: A. Doble et al., Eur. Psychiatry 10, Suppl 3, 117s (1995). Sedative and anxiolytic effects of enantiomers and metabolite in rats: J. N. Carlson et al., Eur. J. Pharmacol. 415, 181 (2001). Series of articles on pharmacokinetics, pharmacology and efficacy in insomnia: Sleep 10, Suppl 1, 1-87 (1987). Clinical overview: B. Musch, F. Maillard, Int. J. Clin. Psychopharmacol. 5, 147-158 (1990). Review of pharmacology, tolerability and therapeutic efficacy: S. Noble et al., Drugs 55, 277-302 (1998).

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