RT Journal Article
SR Electronic
T1 Studies on the Relationship of γ-Aminobutyric Acid-Stimulated Diazepam Binding and the γ-Aminobutyric Acid Receptor
JF Molecular Pharmacology
JO Mol Pharmacol
FD American Society for Pharmacology and Experimental Therapeutics
SP 16
OP 21
VO 20
IS 1
A1 PAUL J. MARANGOS
A1 ANDREA M. MARTINO
YR 1981
UL http://molpharm.aspetjournals.org/content/20/1/16.abstract
AB The three binding parameters [3H]muscimol binding, [3H]diazepam binding, and γ-aminobutyric acid (GABA)-stimulated [3H]diazepam binding are compared in various brain areas and in response to various protein and membrane modifying reagents. Comparison of rat forebrain and cerebellum revealed a much higher ratio of [3H]muscimol- to [3H]diazepam-binding sites in cerebellum and less GABA-stimulated [3H]diazepam binding. Both sulfhydryl reducing and alkylating agents reduced [3H]muscimol binding (decreased binding affinity), and increased GABA-stimulated [3H]diazepam binding. Triton X-100-treated membranes display an increase in both the number and affinity of [3H]muscimol-binding sites, no change in basal [3H]diazepam binding, and a decrease in GABA-stimulated [3H]diazepam binding. The observed relationship between [3H]-muscimol-binding sites and the degree of GABA-stimulated [3H]diazepam binding suggests that the high affinity muscimol-binding site is not mediating the GABA enhancement effect.