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