Hyttel J
Psychopharmacology (Berl). 1979 Oct;65(2):211-4. doi: 10.1007/BF00433051.
Characteristics of 3H-GABA binding to rat brain synaptic membranes in vitro have been investigated. The specific binding of 3H-GABA displays saturation kinetics. Only one single population of receptor sites was found (Km = 31.3 nM) with a concentration of 2.09 pmol/mg protein. Only GABA agonists show inhibitory effect on the binding, whereas GABA antagonists, GABA-uptake inhibitors, and inhibitors of GAD and GABA-T are without effect. The order of potencies for GABA agonists are: Muscimol greater than GABA greater than or equal to 4,5-dihydromuscimol greater than 3-aminoproprane sulphonic acid greater than isoguvacine greater than THIP greater than 3-hydroxy-GABA greater than imidazol-4-acetic acid. Agonists and antagonists from other neurone systems as well as neuroleptics and benzodiazepines had no or only a very slight potency in the binding test.
已对体外3H-GABA与大鼠脑突触膜的结合特性进行了研究。3H-GABA的特异性结合呈现饱和动力学。发现只有一类单一的受体位点（Km = 31.3 nM），蛋白浓度为2.09 pmol/mg。只有GABA激动剂对结合有抑制作用，而GABA拮抗剂、GABA摄取抑制剂以及GAD和GABA-T的抑制剂则无作用。GABA激动剂的效力顺序为：蝇蕈醇大于GABA大于或等于4,5-二氢蝇蕈醇大于3-氨基丙烷磺酸大于异鹅膏蕈氨酸大于四氢异喹啉大于3-羟基-GABA大于咪唑-4-乙酸。来自其他神经元系统的激动剂和拮抗剂以及抗精神病药物和苯二氮䓬类药物在结合试验中无作用或只有非常轻微的效力。
