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The mechanism of action of zopiclone

11/24/2014
07:26 | Author: Devin Garcia

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The mechanism of action of zopiclone

The mechanism of action of the cyclopyrrolone hypnotic drug zopiclone involves allosteric modulation of the GABAA receptor. Zopiclone displaces the binding of.

Studies with protein-modifying agents (eg diethylpyrocarbonate) and photoaffinity labelling suggest that cyclopyrrolones bind to a domain on the GABAA receptor different from the benzodiazepine binding domain. Subchronic treatment of mice with high doses of zopiclone does not produce the changes in sensitivity of the GABAA receptor that are observed with hypnotic benzodiazepines. Zopiclone displaces the binding of -flunitrazepam with an affinity of 28 nM, and enhances the binding of the channel blocker -TBPS. The consequence of this interaction with the GABAA receptor is to potentiate responses to GABA, as can be demonstrated by electrophysiological methods. The mechanism of action of the cyclopyrrolone hypnotic drug zopiclone involves allosteric modulation of the GABAA receptor. The binding of zopiclone, unlike that of hypnotic benzodiazepines, is not facilitated by GABA. Zopiclone does not distinguish between GABAA receptors containing different alpha-subunits (BZ(1) and BZ(2) phenotype).

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Zopiclone - NeuroLex

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03:38 | Author: Evan Martin

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Zopiclone - NeuroLex

Description: Zopiclone is a novel hypnotic agent used in the treatment of insomnia. Its mechanism of action is based on modulating benzodiazepine receptors.

Last modified date : Version number : 287249 Comment : taken from DrugBank Curator (s): ab Ccdbuser, Nifbot2.

Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. While Zopiclone is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. In addition to zopiclone's benzodiazepine pharmacological properties it also has some barbiturate like properties. Zopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor. Name : Zopiclone Description : Zopiclone is a novel hypnotic agent used in the treatment of insomnia. Drug type: Approved. Drug category: Hypnotics and Sedatives Synonym(s) : (+-)-zopiclone, Zopiclona (INN-Spanish), Zopiclone (Ban:Inn:Jan), Zopiclonum (INN-Latin), Amoban, Amovane, Imovance, Imovane, Novo-zopiclone, Nu-Zopiclone, Ran-zopiclone, Rhovane, Sopivan, Ximovan, Zimovane Has role : Drug Super-category : Molecular entity URL : http://www.drugbank.ca/drugs/DB01198 *Id : DB01198 Related to : Translocator protein Link to OWL / RDF : Download this content as OWL/RDF. Small Molecule. Its mechanism of action is based on modulating benzodiazepine receptors. Pharmacology: Zopiclone is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. Mechanism of action: Zopiclone exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABABZ receptor chloride channel macromolecular complex.

Neurons Brain Regions MediaWiki Edit source Zopiclone.

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