Thal L, Creese I, Snyder S H
Eur J Pharmacol. 1978 Jun 1;49(3):295-9. doi: 10.1016/0014-2999(78)90105-x.
3H-apomorphine binds to membranes from areas of the corpus striatum and limbic system of calf brain saturable and with a drug specificity indicating that it labels dopamine receptors. In terms of drug specificity, log-logit displacement curve slopes and number of binding sites, 3H-apomorphine interacts with receptors in a manner more like 3H-dopamine than 3H-haloperidol. These properties of 3H-apomorphine binding are those of an apparently "pure" agonist in contrast to the partial agonist effects of apomorphine upon the dopamine-sensitive adenylate cyclase.
3H-阿扑吗啡可饱和地结合于小牛脑纹状体和边缘系统区域的膜上,且具有药物特异性,表明它标记了多巴胺受体。就药物特异性、对数-对数转换位移曲线斜率和结合位点数量而言,3H-阿扑吗啡与受体的相互作用方式更类似于3H-多巴胺,而非3H-氟哌啶醇。与阿扑吗啡对多巴胺敏感的腺苷酸环化酶的部分激动剂作用相反,3H-阿扑吗啡结合的这些特性是一种明显“纯粹”激动剂的特性。