Article date: 1985/7/1
PubMed ID: 2860208
Journal name: Journal of neurochemistry (ISSN: 0022-3042)
The effects of muscimol and/or incubation temperature on the inhibition of [3H]flunitrazepam receptor binding by benzodiazepine receptor ligands were investigated. At 0 degree C muscimol decreased the Ki values for some ligands as displacers of [3H]flunitrazepam binding to brain-specific sites while increasing or having no effect on the Ki values for other ligands. The Ki values for some ligands are higher at 37 degrees C than at 0 degree C but are reduced by muscimol at both 0 degrees and 37 degrees C. In contrast, the ligands whose Ki values are increased by muscimol either decreased or did not alter the Ki values at 37 degrees C as compared to those at 0 degree C. Incubation of membranes at 37 degrees C for 30 min accelerated gamma-aminobutyric acid (GABA) release by 221% over that at 0 degree C. These results indicate that changes in incubation temperature alter benzodiazepine receptor affinity for ligands via GABA.
Author List: Chweh A Y, Swinyard E A, Wolf H H
Publication Types: Journal Article; Research Support, U.S. Gov't, P.H.S.
Substances mentioned in the article: Anti-Anxiety Agents; Receptors, GABA-A; Muscimol; gamma-Aminobutyric Acid; Flunitrazepam;
Mesh terms: Animals; Anti-Anxiety Agents/pharmacology; Cell Membrane/metabolism; Diencephalon/metabolism; Flunitrazepam/metabolism; Mice; Muscimol/pharmacology; Receptors, GABA-A/drug effects; Telencephalon/metabolism; Temperature; gamma-Aminobutyric Acid/metabolism;