De Vries D J, Beart P M
Eur J Pharmacol. 1985 Mar 12;109(3):417-9. doi: 10.1016/0014-2999(85)90406-6.
Preparation and assay of rat striatal membranes in the presence of 10 mM magnesium ions resulted in an IC50 value constant for dopamine of 13 nM at D-2 dopamine receptors labelled by [3H]spiperone. Inclusion of 100 microM GTP under these conditions resulted in a 13 fold decrease in dopamine displacing potency. Displacing potencies for dopamine in the nanomolar range are associated with agonist-specific D-3 receptor binding and it is predicted that the component of D-2 binding with high agonist affinity may play a confounding role in many D-3 receptor studies.
在存在10 mM镁离子的情况下制备和测定大鼠纹状体膜,结果显示,在用[3H]螺哌隆标记的D-2多巴胺受体上,多巴胺的IC50值恒定为13 nM。在这些条件下加入100 microM GTP,会导致多巴胺置换能力降低13倍。纳摩尔范围内多巴胺的置换能力与激动剂特异性D-3受体结合有关,预计在许多D-3受体研究中,具有高激动剂亲和力的D-2结合成分可能会起到混淆作用。