Hirsch J D
Pharmacol Biochem Behav. 1982 Feb;16(2):245-8. doi: 10.1016/0091-3057(82)90156-3.
When the benzodiazepine receptor in mouse cerebellar, striatal, and hippocampal membranes was photoaffinity labeled with nonradioactive flunitrazepam, specific [3H]diazepam binding determined with either unlabeled diazepam or ethyl beta-carboline-3-carboxylate (betaCCE) as displacer declined greater than 80%. In contrast, specific propyl beta-carboline-3-carboxylate (PrCC) binding in these regions determined with betaCCE as displacer was basically unaltered after photolabeling. Photolabeling lowered specific [3H]PrCC binding with diazepam as displacer to an intermediate extent in the three regions. In cerebellum photolabeling had little effect on either the Kd or Bmax for specific [3H]PrCC binding determined with betaCCE as displacer but significantly lowered the Bmax for specific [3H]PrCC binding determined with diazepam as displacer. These results do not support the idea that [3H]PrCC and [3H]diazepam have a common recognition site on the benzodiazepine receptor. Instead, they suggest that the benzodiazepine receptor is a multicomponent complex.
当用非放射性氟硝西泮对小鼠小脑、纹状体和海马膜中的苯二氮䓬受体进行光亲和标记时,以未标记的地西泮或β-咔啉-3-羧酸乙酯(βCCE)作为置换剂测定的特异性[³H]地西泮结合下降超过80%。相比之下,在这些区域以βCCE作为置换剂测定的特异性丙基β-咔啉-3-羧酸酯(PrCC)结合在光标记后基本未改变。光标记使以地西泮作为置换剂的特异性[³H]PrCC结合在这三个区域中度降低。在小脑中,光标记对以βCCE作为置换剂测定的特异性[³H]PrCC结合的解离常数(Kd)或最大结合容量(Bmax)影响很小,但显著降低了以地西泮作为置换剂测定的特异性[³H]PrCC结合的Bmax。这些结果不支持[³H]PrCC和[³H]地西泮在苯二氮䓬受体上有共同识别位点的观点。相反,它们表明苯二氮䓬受体是一种多组分复合物。