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马吲哚和苯丙胺作为大鼠纹状体突触体对3H-多巴胺摄取及释放的抑制剂。

Mazindol and amphetamine as inhibitors of the uptake and releasers of 3H-dopamine by rat striatal synaptosomes.

作者信息

Carruba M O, Picotti G B, Zambotti F, Mantegazza P

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1977 May;298(1):1-5. doi: 10.1007/BF00510979.

DOI:10.1007/BF00510979
PMID:882144
Abstract

The effects of mazindol, amphetamine and fenfluramine on uptake and release of 3H-DA by synaptosomes were studied in different systems. In in vitro incubations of 3H-DA with synaptosomes isolated from the caudate nucleus of the rat, mazindol inhibited the uptake of the radioactivity more potently than did amphetamine. When the synaptosomes were isolated from the caudate nuclei of rats treated in vivo with either mazindol or amphetamine, the uptake of 3H-DA during in vitro incuation was lower with synaptosomes of amphetamine-treated rats than with those of mazindol-treated rats. When synaptosomes of untreated rats were prelabelled with 3H-DA and incubated in the presence of amphetamine or of mazindol, amphetamine caused a greater release of radioactivity than did mazindol. Fenfluramine was without activity in all these systems. In spite of the quantitative differences, both amphetamine and mazindol appear to have similar effects on uptake and release of dopamine, and this may account for their analogous pharmacological profile.

摘要

在不同系统中研究了马吲哚、苯丙胺和芬氟拉明对突触体摄取和释放3H-多巴胺(3H-DA)的影响。在大鼠尾状核分离的突触体与3H-DA进行体外孵育时,马吲哚比苯丙胺更有效地抑制放射性物质的摄取。当突触体从体内用马吲哚或苯丙胺处理的大鼠的尾状核中分离出来时,在体外孵育期间,苯丙胺处理大鼠的突触体对3H-DA的摄取低于马吲哚处理大鼠的突触体。当未处理大鼠的突触体用3H-DA预先标记并在苯丙胺或马吲哚存在下孵育时,苯丙胺比马吲哚引起更大的放射性物质释放。芬氟拉明在所有这些系统中均无活性。尽管存在定量差异,但苯丙胺和马吲哚对多巴胺的摄取和释放似乎具有相似的作用,这可能解释了它们类似的药理学特征。

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