Article date: 1987/2/1
PubMed ID: 3035415
Journal name: Neuropharmacology (ISSN: 0028-3908)
Modulation of the benzodiazepine receptor/GABA receptor/chloride ionophore complex in vivo involves a number of intricate regulatory interactions between the three components of the receptor complex. One way to assess these potential interactions involves the in vivo labelling of the benzodiazepine receptor with [3H]flunitrazepam. In these studies, we used this approach to demonstrate that the neuroleptic, clozapine, increases [3H]flunitrazepam binding in mouse brain in a bicuculline-reversible manner. This potentiation of benzodiazepine binding was not antagonized by picrotoxin and was found to result from a slower dissociation of [3H]flunitrazepam from the benzodiazepine receptor. These data suggest that clozapine acts to increase [3H]flunitrazepam binding via a GABAergic mechanism, independent of the chloride channel.
Author List: McPherson S E, Loo P, Braunwalder A, Wood P L
Publication Types: Journal Article
Substances mentioned in the article: Dibenzazepines; Receptors, GABA-A; Muscimol; Flunitrazepam; Clozapine; Bicuculline;
Mesh terms: Animals; Bicuculline/pharmacology; Brain/drug effects; Clozapine/pharmacology; Dibenzazepines/pharmacology; Drug Interactions; Flunitrazepam/metabolism; Male; Mice; Muscimol/pharmacology; Receptors, GABA-A/drug effects;