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某些氨基四氢萘从大鼠纹状体切片中释放放射性标记的多巴胺、对酪胺和间酪胺。

Release of radiolabeled dopamine, p-tyramine, and m-tyramine from rat striatal slices by some aminotetralins.

作者信息

Dyck L E

出版信息

Neurochem Res. 1981 Apr;6(4):365-75. doi: 10.1007/BF00963851.

Abstract

The effect of several 2-aminotetralins (2ATs) on the uptake and release of [14C] dopamine and [2H]m- or [3H]p-tyramine by rat striatal slices was examined. 6,7-Dihydroxy-2AT (6,7OHAT) and 5,6-dihydroxy-2-methyl-AT (5,6OHMeAT) were the most potent uptake inhibitors as well as the most potent releasers of the three labeled amines. The 5-, 6-, and 7-hydroxy-2-N, N-dipropyl-ATs (5-, 6-, and 7OHdiPrAT) and 5,6-dihydroxy-2-N,N-dipropyl-AT (5,6OHdiPrAT) significantly inhibited the uptakes of the three labeled amines, but they released only the tyramines. The dipropyl substitutions of a 2AT appeared to confer a tyraminergic specificity to its release properties. To verify this supposition, 2AT was compared to 2-N,N-dipropyl-AT (diPrAT). Although 2AT released both [3H]p-tyramine and [14C]dopamine, diPrAT released only [3H]p-tyramine. None of the compounds, however, differentiated between m- and p-tyramine. It was concluded that the release of tyramines could be implicated in the actions of some of the 2ATs and that the tyramines can be transported independently from dopamine.

摘要

研究了几种2-氨基四氢萘(2ATs)对大鼠纹状体切片摄取和释放[14C]多巴胺以及[2H]间酪氨酸或[3H]对酪氨酸的影响。6,7-二羟基-2AT(6,7OHAT)和5,6-二羟基-2-甲基-AT(5,6OHMeAT)是三种标记胺类最强效的摄取抑制剂,也是最强效的释放剂。5-、6-和7-羟基-2-N,N-二丙基-ATs(5-、6-和7OHdiPrAT)以及5,6-二羟基-2-N,N-二丙基-AT(5,6OHdiPrAT)显著抑制了三种标记胺类的摄取,但它们只释放酪氨酸。2AT的二丙基取代似乎赋予了其释放特性酪氨酸能特异性。为了验证这一假设,将2AT与2-N,N-二丙基-AT(diPrAT)进行了比较。虽然2AT释放了[3H]对酪氨酸和[14C]多巴胺,但diPrAT只释放了[3H]对酪氨酸。然而,没有一种化合物能区分间酪氨酸和对酪氨酸。得出的结论是,酪氨酸的释放可能与某些2ATs的作用有关,并且酪氨酸可以独立于多巴胺进行转运。

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