McAllister G, Knowles M R, Patel S, Marwood R, Emms F, Seabrook G R, Graziano M, Borkowski D, Hey P J, Freedman S B
Neuroscience Research Centre, Merck, Sharp and Dohme Research Laboratories, Harlow, Essex, UK.
FEBS Lett. 1993 Jun 7;324(1):81-6. doi: 10.1016/0014-5793(93)81537-a.
The D2 dopamine receptor is known to be functionally coupled when expressed in CHO cells, whereas the effector systems for the D3 dopamine receptor remain unclear. A chimeric, human D3/D2 receptor (hD3/D2) was constructed containing the third intracellular loop region of the D2 receptor. CHO cells stably expressing the D2, D3, or hD3/D2 receptors were created and the pharmacology of the receptors was examined. The chimeric hD3/D2 receptor retained D3-like affinities for dopaminergic ligands. However, in contrast to the D2 receptor neither the D3 receptor nor the hD3/D2 receptor could functionally couple to the adenylate cyclase or arachidonic acid release mechanisms.
已知D2多巴胺受体在CHO细胞中表达时会发生功能偶联，而D3多巴胺受体的效应系统仍不清楚。构建了一种嵌合的人D3/D2受体（hD3/D2），其包含D2受体的第三个细胞内环区域。创建了稳定表达D2、D3或hD3/D2受体的CHO细胞，并检测了这些受体的药理学特性。嵌合的hD3/D2受体对多巴胺能配体保留了类似D3的亲和力。然而，与D2受体不同，D3受体和hD3/D2受体均不能与腺苷酸环化酶或花生四烯酸释放机制发生功能偶联。
