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Molecular Pharmacology, Vol 13, 442-453, Copyright © 1977 by the American Society for Pharmacology and Experimental Therapeutics
-Aminobutyric Acid-Receptor Binding in Synaptic Membranes of Rat Brain
1 Departments of Pharmacology and Experimental Therapeutics and Psychiatry and the Behavioral Sciences,
The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205
The effects of ions, detergents, and enzymes on
-aminobutyric acid (GABA) binding to
synaptic receptor sites in membranes of rat brain in the absence of sodium is contrasted
with influences on sodium-dependent GABA binding. The anions thiocyanate, iodide,
and nitrate increase the potency of the GABA antagonist bicuculline 10-fold in inhibiting sodium-independent GABA-receptor binding without affecting the potency of GABA
agonists. Very low concentrations of the detergent Triton X-100 increase sodium-independent GABA-receptor binding up to 5-fold. In the presence of Triton X-100,
GABA-receptor binding can be detected with considerable sensitivity using fresh or
previously frozen tissue in the presence of sodium, facilitating studies of GABA receptors in small tissue samples and increasing the sensitivity of radioreceptor assays for
endogenous GABA.
Note:
ACKNOWLEDGMENTS
We thank Ms. Cindy Kaufman and Mr. Harold
Frank for their technical assistance.
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