CHARACTERIZATION OF THE BINDING OF [MUSCIMOL-H-3, A POTENT GAMMA-AMINOBUTYRIC ACID AGONIST, TO RAT-BRAIN SYNAPTOSOMAL MEMBRANES USING A FILTRATION ASSAY

被引:147
作者
WILLIAMS, M
RISLEY, EA
机构
[1] Neuropsychopharmacology Section, Merck Institute for Therapeutic Research West Point, Pennsylvania
关键词
D O I
10.1111/j.1471-4159.1979.tb04553.x
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Abstract— The binding of [3H]muscimol, a potent GABA agonist, to crude synaptic membranes prepared from rat brain was studied using a filtration method to isolate membrane‐bound ligand. Specific binding was found to be saturable and occurred to two binding sites of Kd5 5 and 30 nm. Binding was Na+‐independent and enhanced by both freezing and Triton treatment. Regional and subcellular distribution studies and pharmacological characterization of specific [3H]muscimol binding are consistent with binding to the synaptic GABA receptor. Copyright © 1979, Wiley Blackwell. All rights reserved
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页码:713 / 718
页数:6
相关论文
共 22 条
[1]   MUSCIMOL BINDING IN RAT-BRAIN - ASSOCIATION WITH SYNAPTIC GABA RECEPTORS [J].
BEAUMONT, K ;
CHILTON, WS ;
YAMAMURA, HI ;
ENNA, SJ .
BRAIN RESEARCH, 1978, 148 (01) :153-162
[2]  
BENNETT JP, 1978, NEUROTRANSMITTER REC, P57
[3]   COMPARISON OF GAMMA-AMINOBUTYRIC ACID AND SEMI-RIGID ANALOGS 4-AMINOTETROLIC ACID, 4-AMINOCROTONIC ACID AND IMIDAZOLE-4-ACETIC ACID ON ISOLATED SUPERIOR CERVICAL GANGLION OF RAT [J].
BOWERY, NG ;
JONES, GP .
BRITISH JOURNAL OF PHARMACOLOGY, 1976, 56 (03) :323-330
[4]  
DRAPER NR, 1966, APPLIED REGRESSION A, P67
[5]   STEREOSPECIFICITY AND STRUCTURE-ACTIVITY REQUIREMENTS OF GABA RECEPTOR-BINDING IN RAT-BRAIN [J].
ENNA, SJ ;
COLLINS, JF ;
SNYDER, SH .
BRAIN RESEARCH, 1977, 124 (01) :185-190
[6]  
ENNA SJ, 1977, MOL PHARMACOL, V13, P442
[7]   PROPERTIES OF GAMMA-AMINOBUTYRIC ACID (GABA) RECEPTOR-BINDING IN RAT-BRAIN SYNAPTIC MEMBRANE-FRACTIONS [J].
ENNA, SJ ;
SNYDER, SH .
BRAIN RESEARCH, 1975, 100 (01) :81-97
[8]   REGIONAL STUDIES OF CATECHOLAMINES IN RAT BRAIN .I. DISPOSITION OF [3H]NOREPINEPHRINE [3H]DOPAMINE AND [3H]DOPA IN VARIOUS REGIONS OF BRAIN [J].
GLOWINSKI, J ;
IVERSEN, LL .
JOURNAL OF NEUROCHEMISTRY, 1966, 13 (08) :655-+
[9]  
GOLDSTEIN A, 1974, PRINCIPLES DRUG ACTI, P47
[10]   NEUROPHARMACOLOGY OF AMINO-ACID INHIBITORY TRANSMITTERS [J].
JOHNSTON, GAR .
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, 1978, 18 :269-289