GABAa receptors, activation benzodiazepine binding site

The pyridoacridine alkaloids isolated from the Micronesian sponge Oceanapia sp. were tested for insecticidal activity, cytotoxicity properties, as well as for their ability to bind to adenosine receptors and to benzodiazepine binding sites of GABAa receptors [91]. Kuanoniamines C... 

Dekermendjian, K. et al., Structure-activity relationships and molecular modeling analysis of flavonoids binding to the benzodiazepine site of the rat brain GABAa receptor complex, J. Med. Chem., 42, 4343, 1999. 

Zolpidem (an imidazopyridine), zale-plone (a pyrazolopyrimidine) and zopi-clone (a cyclopyrrolone) are hypnotics that, despite their different chemical structure, can bind to the benzodiazepine site on the GABAa receptor (p. 222). However, their effects do not appear to be identical to those of benzodiazepines. Thus, compared with benzodiazepines, zolpidem exerts a weaker effect on sleep phases, supposedly carries a lower risk of dependence, and appears to have less anxiolytic activity. Heterogeneity of GABAa receptors may explain these differences in activity. GABAa receptors consist of five subunits that exist in several subtypes. 

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