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γ‐Aminobutyric Acid: Temperature Dependence in Benzodiazepine Receptor Binding
Author(s) -
Chweh Andrew Y.,
Swinyard Ewart A.,
Wolf Harold H.
Publication year - 1985
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1985.tb05499.x
Subject(s) - muscimol , flunitrazepam , incubation , chemistry , gabaa receptor , benzodiazepine , aminobutyric acid , receptor , agonist , binding site , biochemistry , stereochemistry
The effects of muscimol and/or incubation temperature on the inhibition of [ 3 H]flunitrazepam receptor binding by benzodiazepine receptor ligands were investigated. At 0°C muscimol decreased the K i values for some ligands as displacers of [ 3 H]flunitrazepam binding to brain‐specific sites while increasing or having no effect on the K i values for other ligands. The K i values for some ligands are higher at 37°C than at 0°C but are reduced by muscimol at both 0° and 37°C. In contrast, the ligands whose K t values are increased by muscimol either decreased or did not alter the K i values at 37°C as compared to those at 0°C. Incubation of membranes at 37°C for 30 min accelerated γ‐aminobutyric acid (GABA) release by 221% over that at 0°C. These results indicate that changes in incubation temperature alter benzodiazepine receptor affinity for ligands via GABA.