Burt D R, Enna S J, Creese I, Snyder S H
Proc Natl Acad Sci U S A. 1975 Nov;72(11):4655-9. doi: 10.1073/pnas.72.11.4655.
Specific binding of [3H]dopamine to membranes from the corpus striatum of rat and calf brain appears to involve the postsynaptic dopamine receptor. Specific [3H]dopamine binding is saturable, wnd with half-maximal binding in calf membranes at 7 nM. Apomorphine is about twice as potent as dopamine in competing for binding sites, whereas (-)norepinephrine is 5% as potent as dopamine and isoproterenol is virtually inactive. The relative potencies of phenothiazines as inhibitors of specific dopamine binding correlates with their clinical potencies and actions on the dopamine-sensitive adenylate cyclase.
[3H]多巴胺与大鼠和小牛脑纹状体膜的特异性结合似乎涉及突触后多巴胺受体。特异性[3H]多巴胺结合是可饱和的,小牛膜中半数最大结合浓度为7 nM。阿扑吗啡在竞争结合位点方面的效力约为多巴胺的两倍,而(-)去甲肾上腺素的效力为多巴胺的5%,异丙肾上腺素实际上无活性。吩噻嗪类作为特异性多巴胺结合抑制剂的相对效力与其临床效力以及对多巴胺敏感的腺苷酸环化酶的作用相关。