源自顺式和反式八氢苯并[f]喹啉以及反式八氢苯并[g]喹啉的多巴胺β构象异构体的同系物。

Congeners of the beta conformer of dopamine derived from cis- and trans-octahydrobenzo[f]quinoline and trans-octahydrobenzo[g]quinoline.

作者信息

Cannon J G, Lee T, Goldman H D, Long J P, Flynn J R, Verimer T, Costall B, Naylor R J

出版信息

J Med Chem. 1980 Jan;23(1):1-5. doi: 10.1021/jm00175a001.

Abstract

The so-called beta conformer of dopamine has been proposed to be involved in agonist--receptor interactions at several sites in the dopaminergic nervous system. Further to evaluate this proposal, rigid congeners of the beta conformer derived from linearly and angularly annelated octahydrobenzoquinolines have been synthesized. Certain N-alkylated trans-angularly annelated systems exhibited unusually potent and highly selective dopamine-like effects in an assay on a cardioaccelerator nerve preparation in the cat, but these compounds were inactive in a variety of assays for CNS effects. These compounds present a clear separation of CNS effects from some potent peripheral effects.

摘要

多巴胺的所谓β构象异构体已被提出参与多巴胺能神经系统多个位点的激动剂与受体相互作用。为进一步评估这一观点，已合成了源自线性和角形稠合八氢苯并喹啉的β构象异构体的刚性类似物。某些N-烷基化的反式角形稠合体系在猫的心脏加速神经制剂试验中表现出异常强效且高度选择性的多巴胺样作用，但这些化合物在多种中枢神经系统效应试验中无活性。这些化合物显示出中枢神经系统效应与一些强效外周效应的明显分离。