Hirschhorn I D, Makman M H
Eur J Pharmacol. 1982 Sep 10;83(1-2):61-7. doi: 10.1016/0014-2999(82)90286-2.
The present experiments examined some characteristics of the enhanced striatal [3H]ADTN binding which occurs following substantia nigra lesion. The amount of binding of a fixed concentration of [3H]ADTN was greatly increased. The amount of guanine nucleotide sensitivity increased to an even greater extent than total [3H]ADTN binding. Saturation experiments showed one component of [3H]ADTN binding (KD 7 nM) in intact striata whereas there were two components of binding (KD 9 nM and KD 1 nM) in substantia nigra-lesioned striata. Most of the enhanced binding in substantia nigra-lesioned striata was the higher affinity component. Kainic acid lesion of substantia nigra-lesioned striata caused loss of the enhanced [3H]ADTN binding and the high affinity component of [3H]ADTN binding. These results indicate that following dopaminergic denervation, either the binding characteristics of a single type of dopamine receptor are altered or there is a specific increase in a distinct subtype of dopamine receptor with high agonist affinity and sensitivity to guanine nucleotides.
本实验研究了黑质损伤后纹状体中增强的[3H]ADTN结合的一些特征。固定浓度的[3H]ADTN的结合量大幅增加。鸟嘌呤核苷酸敏感性的增加幅度甚至超过了总的[3H]ADTN结合量。饱和实验表明,完整纹状体中[3H]ADTN结合有一个成分(解离常数KD为7 nM),而在黑质损伤的纹状体中有两个结合成分(KD分别为9 nM和1 nM)。黑质损伤的纹状体中增强的结合大多是高亲和力成分。对黑质损伤的纹状体进行 kainic 酸损伤会导致增强的[3H]ADTN结合以及[3H]ADTN结合的高亲和力成分丧失。这些结果表明,在多巴胺能去神经支配后,要么单一类型多巴胺受体的结合特性发生改变,要么具有高激动剂亲和力和对鸟嘌呤核苷酸敏感性的不同多巴胺受体亚型出现特异性增加。