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R-SK与F 38393对纹状体D1和D2多巴胺受体的[3H]匹莫齐特结合而非[3H]螺哌隆结合的选择性和立体特异性相互作用：与SCH 23390的比较。

Selective and stereospecific interactions of R-SK & F 38393 with [3H]piflutixol but not [3H]spiperone binding to striatal D1 and D2 dopamine receptors: comparisons with SCH 23390.

作者信息

O'Boyle K M, Waddington J L

出版信息

Eur J Pharmacol. 1984 Mar 2;98(3-4):433-6. doi: 10.1016/0014-2999(84)90294-2.

DOI:10.1016/0014-2999(84)90294-2
PMID:6144559
Abstract

Four benzazepine derivatives, racemic SK&F 38393, its resolved R- and S-enantiomers, and SCH 23390 have been investigated for their interactions with striatal D1 and D2 dopamine receptors, as indexed by the binding of [3H] piflutixol and [3H]spiperone respectively. For the agonist SK&F 38393, its R-enantiomer was active in displacing [3H] piflutixol while its S- antipode was 100 fold less potent. In contrast, both enantiomers showed similar and negligible activity to displace [3H]spiperone. SCH 23390, an antagonist analogue with an R-configuration, potently displaced [3H] piflutixol but not [3H]spiperone. R-SK&F 38393 and SCH 23390 may help clarify the structural requirements for, and functional consequences of, selective actions at the D1 dopamine receptor.

摘要

已对四种苯并氮杂䓬衍生物，即消旋体SK&F 38393、其拆分后的R-和S-对映体以及SCH 23390，研究了它们与纹状体D1和D2多巴胺受体的相互作用，分别以[3H]匹氟噻吨和[3H]螺哌隆的结合作为指标。对于激动剂SK&F 38393，其R-对映体在置换[3H]匹氟噻吨方面具有活性，而其S-对映体的效力则低100倍。相反，两种对映体在置换[3H]螺哌隆方面均表现出相似且可忽略不计的活性。SCH 23390是一种具有R-构型的拮抗剂类似物，能有效置换[3H]匹氟噻吨，但不能置换[3H]螺哌隆。R-SK&F 38393和SCH 23990可能有助于阐明对D1多巴胺受体选择性作用的结构要求及其功能后果。

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