强效γ-氨基丁酸受体激动剂[3H]-蝇蕈醇与牛视网膜膜的结合。
Binding of [3H]-muscimol, a potent gamma-aminobutyric acid receptor agonist, to membranes of the bovine retina.
作者信息
Osborne N N
出版信息
Br J Pharmacol. 1980;71(1):259-64. doi: 10.1111/j.1476-5381.1980.tb10934.x.
Abstract
1 The binding of [3H]-muscimol, a potent gamma-aminobutyric acid (GABA) receptor agonist, to crude membrane preparations of bovine retina was studied, using a filtration method to isolate membrane-bound ligand. 2 Specific binding was found to be saturable and occurred at two binding sites with affinity constants of 4.3 nM and 38.2 nM. 3 Binding was sodium-independent, enhanced by both freezing and Triton X-100 treatment but abolished with sodium laurylsulphate. 4 The binding sites demonstrated a high degree of pharmacological specificity, GABA being a potent displacer of [3H]-muscimol. 5 A higher degree of [3H]-muscimol binding was associated with subcellular fractions enriched with photoreceptor synaptosomes rather than with fractions enriched with conventional synaptosomes.
摘要
- 采用过滤法分离膜结合配体，研究了强效γ-氨基丁酸（GABA）受体激动剂[3H]-蝇蕈醇与牛视网膜粗膜制剂的结合情况。2. 发现特异性结合具有饱和性，且在两个结合位点发生，其亲和常数分别为4.3 nM和38.2 nM。3. 结合不依赖于钠，冷冻和Triton X-100处理均可增强结合，但十二烷基硫酸钠可使其消除。4. 结合位点表现出高度的药理学特异性，GABA是[3H]-蝇蕈醇的强效置换剂。5. [3H]-蝇蕈醇的较高结合程度与富含光感受器突触小体的亚细胞组分相关，而非与富含传统突触小体的组分相关。
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1
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2
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3
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4
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5
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