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[血脑屏障。II. 大鼠静脉注射3H-对羟基苯丙胺后在脑结构中的分布动力学]

[Blood-brain barrier. II. Kinetics of distribution of 3H-parahydroxyamphetamine in brain structures after intravenous administration in the rat].

作者信息

Lindenbaum A, Marcher K, Wepierre J, Cohen Y

出版信息

Arch Int Pharmacodyn Ther. 1975 May;215(1):168-76.

PMID:1164084
Abstract

Intravenously injected parahydroxyamphetamine hardly penetrates into the Central Nervous System, since, 5 minutes after injection, the tissue to plamsa concentration ratio for brain and cerebrospinal fluid amounts to 0,67 and 0,35 respectively. Its concentration in muscle is 5 times higher than in plasma. In the brain, the molecule is preferentialy taken up by the corpus striatum and the hypothalamus. Thus, parahydroxylation of amphetamine inhibits the penetration of the molecule into the brain and suppresses its cortical fixation. These characteristics could explain why this parahydroxylated amine has no psychotropic action.

摘要

静脉注射对羟基苯丙胺很难穿透进入中枢神经系统,因为注射后5分钟,脑和脑脊液的组织与血浆浓度比分别为0.67和0.35。其在肌肉中的浓度比血浆中高5倍。在脑中,该分子优先被纹状体和下丘脑摄取。因此,苯丙胺的对羟基化抑制了分子进入脑内,并抑制其在皮质的固定。这些特性可以解释为什么这种对羟基化胺没有精神活性作用。

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