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Cat. No. Name Size Price Add Cart
KI1367Zopiclone10 mg$250

Chemical Characteristic

Product NameZopiclone
SynonymsImovane, Zimovane, Lunesta, RP 27267
CAS No.43200-80-2
Molecular Weight 388.81
FormulaC17H17ClN6O3
Chemical Name4-Methyl-1-piperazinecarboxylic acid 6-(5-chloro-2-pyridinyl)-6,7-dihydro-7-oxo-5H-pyrrolo[3,4-b]pyrazin-5-yl ester
SmilesN1(CCN(CC1)C)C(=O)OC1c2c(nccn2)C(=O)N1c1ccc(cn1)Cl
Chemical Structure

Biological activities

Zopiclone is a γ-aminobutyric acid receptor agonist. [1] Zopiclone is a non-benzodiazepine hypnotic drug. Zopiclone exhibits anticonvulsant.[2] Zopiclone prevents the binding of [3H] diazepam and [3H] flunitrazepam to brain receptors.[3] Zopiclone has a short half-life of about 5 hours. [2] Zopiclone is metabolised by cytochrome P450 (CYP) 3A4 and 2C8 in vitro.[4] Zopiclone is metabolized into N-desmethyl-zopiclone (ND-Z) and N-oxide-zopiclone (NO-Z) with Km and Vm of 78 and 84 µM, 45 and 54 pmol/min/mg for ND-Z and NO-Z generation, respectively, in human liver microsomes.[5] Intrathecal injection of zopiclone potentiates morphine antinociception. In contrast, the intracerebroventricular injection of zopiclone fails to enhance morphine antinociception.[6]

Protocols

Zopiclone is dissolved in 0.1 N hydrochloric acid in vivo assay.[6]

References

[1] Becquemont L, et al. Cytochrome P-450 3A4 and 2C8 are involved in zopiclone metabolism. Drug Metab Dispos. 1999, 27(9): 1068-1073.
[2] Goa KL, et al. Zopiclone. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy as an hypnotic. Drugs. 1986, 32(1): 48-65.
[3] Blanchard JC, et al. In vitro and in vivo inhibition by zopiclone of benzodiazepine binding to rodent brain receptors. Life Sci. 1979, 24(26): 2417-2420.
[4] Tornio A, et al.The CYP2C8 inhibitor gemfibrozil does not increase the plasma concentrations of zopiclone. Eur J Clin Pharmacol. 2006, 62(8): 645-651.
[5] Becquemont L, et al. Cytochrome P-450 3A4 and 2C8 are involved in zopiclone metabolism. Drug Metab Dispos. 1999, 27(9): 1068-1073.
[6] Zambotti F, et al. Zopiclone potentiates the antinociceptive effect of morphine in rats. Naunyn Schmiedebergs Arch Pharmacol. 1987, 336(5): 526-529.

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