S-(+)-阿朴啡对人D3多巴胺受体没有选择性。
S-(+)-aporphines are not selective for human D3 dopamine receptors.
作者信息
Kula N S, Baldessarini R J, Kebabian J W, Neumeyer J L
机构信息
Mailman Research Center, McLean Division-Massachusetts General Hospital, Belmont 02178.
出版信息
Cell Mol Neurobiol. 1994 Apr;14(2):185-91. doi: 10.1007/BF02090784.
Abstract
- Our aim was to test the hypothesis that selectivity for D3 dopamine (DA) receptors may contribute to limbic anti-DA selectivity of S-(+)-aporphine DA partial agonists. 2. Affinity was tested with 3H-emonapride, using human D3 receptors in mouse fibroblasts and D2 receptors in rat striatal tissue. 3. D3 receptors showed a picomolar affinity for 3H-emonapride, Na+ dependence, and reversible saturability, as well as stereoselectivity. Confirmatory or novel D3/D2 pharmacologic selectivity was found with several benzamides, thioxanthenes, buspirone, GBR-12909, and DA agonists including hydroxyaminotetralins [ADTN, (+)-7-OH-DPAT, (-)-PPHT and its fluorescein derivative], (-)-N-propylnorapomorphine, (-)-3-PPP, (-)-quinpirole, and SDZ-205-502, but neither aminoergoline nor (+)-aporphine partial agonists. 4. The results extend pharmacologic characterization of D3-transfected cell membranes but fail to account for the high limbic anti-DA selectivity of S-(+)-aporphines.
摘要
- 我们的目的是检验以下假设：对D3多巴胺（DA）受体的选择性可能有助于S-(+)-阿朴啡DA部分激动剂的边缘抗DA选择性。2. 使用小鼠成纤维细胞中的人D3受体和大鼠纹状体组织中的D2受体，用3H-依莫必利测试亲和力。3. D3受体对3H-依莫必利表现出皮摩尔亲和力、钠依赖性、可逆饱和性以及立体选择性。在几种苯甲酰胺、硫杂蒽类、丁螺环酮、GBR-12909和DA激动剂（包括羟基氨基四氢萘[ADTN、(+)-7-OH-DPAT、(-)-PPHT及其荧光素衍生物]、(-)-N-丙基去甲阿朴吗啡、(-)-3-PPP、(-)-喹吡罗和SDZ-205-502）中发现了确证性或新型的D3/D2药理选择性，但在氨基麦角林或(+)-阿朴啡部分激动剂中未发现。4. 这些结果扩展了D3转染细胞膜的药理学特征，但未能解释S-(+)-阿朴啡的高边缘抗DA选择性。
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