Draft:Desmethylzopiclone

Desmethylzopiclone, also known as SEP-174559, is an active metabolite of the sedative-hypnotic drug zolpiclone.

Unlike its parent compound, which is a largely non-selective benzodiazepine site agonist, Desmethylzopiclone is a selective partial agonist at the benzodiazepine site of α3-containing GABA receptor subtypes. It is also an antagonist to nicotinic acetylcholine and NMDA receptors.

Desmethylzopiclone has been described as a potential anxio-selective metabolite of zolpicloning owing to its selective affinity for the modulation of α3-containing GABA receptor subtypes. These GABA-A subtypes have been implicated as key mediators of the anxiolytic effects of benzodiazepines.

The quantification of desmethylzopiclone from urine has been demonstrated and may serve useful in forensic analysis of cases involving zolpiclone intoxication.