3058 T3D3016 Zopiclone Zopiclone is only found in individuals that have used or taken this drug. It is a novel hypnotic agent used in the treatment of insomnia. Its mechanism of action is based on modulating benzodiazepine receptors. In addition to zopiclone's benzodiazepine pharmacological properties it also has some barbiturate like properties. Zopiclone exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABA<sub>B</sub>Z receptor chloride channel macromolecular complex. Both zopiclone and benzodiazepines act indiscriminately at the benzodiazepine binding site on &#945;1, &#945;2, &#945;3 and &#945;5 GABA<sub>A</sub> containing receptors as full agonists causing an enhancement of the inhibitory actions of GABA to produce the therapeutic (hypnotic and anxiolytic) and adverse effects of zopiclone. 43200-80-2 5735 C17H17ClN6O3 388.105070 White powder. 178°C 0.151 mg/mL at 25°C Rapidly absorbed following oral administration. Zopiclone exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABA<sub>B</sub>Z receptor chloride channel macromolecular complex. Both zopiclone and benzodiazepines act indiscriminately at the benzodiazepine binding site on alpha1, alpha2, alpha3 and alpha5 GABAA containing receptors as full agonists causing an enhancement of the inhibitory actions of GABA to produce the therapeutic (hypnotic and anxiolytic) and adverse effects of zopiclone. Extensively metabolized in the liver via decarboxylation (major pathway), demethylation, and side chain oxidation. Metabolites include an N-oxide derivative (weakly active; approximately 12% of a dose) and an N-desmethyl metabolite (inactive; approximately 16%). Approximately 50% of a dose is converted to other inactive metabolites via decarboxylation. Hepatic microsomal enzymes are apparently not involved in zopiclone clearance. Half Life: Elimination half life is approximately 5 hours (range 3.8 to 6.5 hours) and is prolonged to 11.9 hours in patients with hepatic insufficiency. No indication of carcinogenicity to humans (not listed by IARC). For the short-term treatment of insomnia. They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive. Rare individual instances of fatal outcomes following overdose with racemic zopiclone have been reported in European postmarketing reports, most often associated with overdose with other CNS-depressant agent. Signs and symptoms of overdose effects of CNS depressants can be expected to present as exaggerations of the pharmacological effects noted in preclinical testing. 2009-07-21T20:28:36Z 2026-03-31T19:06:59Z Zopiclone 32315 Zopiclone DB01198 true CN1CCN(CC1)C(=O)OC1N(C(=O)C2=NC=CN=C12)C1=NC=C(Cl)C=C1 C17H17ClN6O3 InChI=1S/C17H17ClN6O3/c1-22-6-8-23(9-7-22)17(26)27-16-14-13(19-4-5-20-14)15(25)24(16)12-3-2-11(18)10-21-12/h2-5,10,16H,6-9H2,1H3 GBBSUAFBMRNDJC-UHFFFAOYSA-N 388.808 388.105066147 Exogenous Solid 0.8 HMDB15329 CHEMBL135400 5533 <p>Thomas Jerussi, &#8220;Compositions comprising zopiclone derivatives and methods of making and using the same.&#8221; U.S. Patent US20040147521, issued July 29, 2004.</p> CHEM002373 DTXSID4041155 NS00010396 6-(5-chloropyridin-2-yl)-7-oxo-5H,6H,7H-pyrrolo[3,4-b]pyrazin-5-yl 4-methylpiperazine-1-carboxylate