阿扑吗啡非羟基化刚性类似物的多巴胺能效应。

Dopaminergic effects of non-hydroxylated rigid analogs of apomorphine.

作者信息

Rusterholz D B, Long J P, Flynn J R, Cannon J G, Lee T, Pease J P, Clemens J A, Wong D T, Bymaster F P

出版信息

Eur J Pharmacol. 1979 Apr 1;55(1):73-82. doi: 10.1016/0014-2999(79)90149-3.

Abstract

A series of rigid analogs of apomorphine lacking aromatic hydroxyl substitutents were evaluated for dopaminergic properties. Three compounds, N-methyl-N-propyl-2-aminotetralin (Me-Pr-2-AT), N-N-dipropyl-2-aminotetralin (Di-pr-2-AT) and N,N-dipropyl-2-aminoindane (Di-Pr-2-AI) induced emesis in dogs, contralateral circling in unilaterally lesioned rats, and inhibited prolactin secretion. The induced circling responses, however, were attenuated by prior treatment with alpha-methyl-p-tyrosine methyl ester (AMPTME) and the compounds were weak inhibitors of 3-H-dopamine binding in calf caudate homogenates. The possibility that these agents may be metabolically activated in vivo is discussed.

摘要

对一系列缺乏芳香羟基取代基的阿扑吗啡刚性类似物的多巴胺能特性进行了评估。三种化合物，N-甲基-N-丙基-2-氨基四氢萘（Me-Pr-2-AT）、N,N-二丙基-2-氨基四氢萘（Di-pr-2-AT）和N,N-二丙基-2-氨基茚满（Di-Pr-2-AI）在犬中引起呕吐，在单侧损伤的大鼠中引起对侧旋转，并抑制催乳素分泌。然而，预先用α-甲基-p-酪氨酸甲酯（AMPTME）处理可减弱诱导的旋转反应，并且这些化合物是小牛尾状核匀浆中3-H-多巴胺结合的弱抑制剂。讨论了这些药物可能在体内被代谢激活的可能性。