多巴胺D3受体的异构体选择性。
Isomeric selectivity at dopamine D3 receptors.
作者信息
Baldessarini R J, Kula N S, McGrath C R, Bakthavachalam V, Kebabian J W, Neumeyer J L
机构信息
Mailman Research Center, McLean Division of Massachusetts General Hospital.
出版信息
Eur J Pharmacol. 1993 Aug 3;239(1-3):269-70. doi: 10.1016/0014-2999(93)91011-b.
Racemic 7-hydroxy-N,N-dipropylaminotetralin (7-OH-DPAT) shows greater affinity for limbic-selective dopamine D3 receptors than for more ubiquitous dopamine D2 receptors. R(+)-7-OH-DPAT was prepared and evaluated in radioreceptor assays using membranes of fibroblasts expressing the human dopamine D3 receptor as well as rat striatal membranes containing dopamine D2 receptors. This enantiomer had 2-fold greater D3 affinity than the racemate and similarly greater D3 vs. D2 selectivity (64-fold). The results may facilitate development of D3 selective agents and evaluation of functions of these receptors.
消旋7-羟基-N,N-二丙基氨基四氢萘（7-OH-DPAT）对边缘系统选择性多巴胺D3受体的亲和力比对分布更广泛的多巴胺D2受体的亲和力更高。制备了R(+)-7-OH-DPAT，并在放射性受体分析中进行评估，该分析使用表达人多巴胺D3受体的成纤维细胞膜以及含有多巴胺D2受体的大鼠纹状体膜。该对映体对D3受体的亲和力比对消旋体高2倍，对D3受体与D2受体的选择性同样更高（64倍）。这些结果可能有助于开发D3选择性药物以及评估这些受体的功能。
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