Effects of racemic, (S)- and (R)-methylenedioxyamphetamine on synaptosomal uptake and release of tritiated norepinephrine.
Effects of racemic, (S)- and (R)-methylenedioxyamphetamine on synaptosomal uptake and release of tritiated norepinephrine.
复制标题
外消旋、(S)-和(R)-亚甲基二氧基苯丙胺对氚化去甲肾上腺素突触体摄取和释放的影响。
DOI：
10.1016/0006-2952(78)90106-5
复制
发表时间：
1978
影响因子：
5.8
通讯作者：
L. L. Ling
中科院分区：
文献类型：
--
作者：
G. Marquardt;V. Distefano;L. L. Ling
外消旋、（S）-和（R）-亚甲二氧基苯丙胺（MDA）是大鼠下丘脑突触体摄取[~ 3 H]去甲肾上腺素（NE）的强竞争性抑制剂。(S)-和（R）-α-甲基多巴胺是[~ 3 H]去甲肾上腺素摄取的极强竞争性抑制剂，确立了这些化合物是迄今报道的脑NE摄取的最强抑制剂。外消旋的。(S)-和（R）-MDA作为释放剂的效力分别略低于（±）-、（+）-和（-）苯丙胺。(S)-和（R）-α-甲基多巴胺是所检测的最有效的释放剂。
Racemic, (S)- and (R)-methylenedioxyamphetamine (MDA) were potent competitive inhibitors of [3H]norepinephrine (NE) uptake by rat hypothalamic synaptosomes. (S)- and (R)-α-methyldopamine were extremely potent competitive inhibitors of [3H]norepinephrine uptake, establishing these compounds as the most potent inhibitors of brain NE uptake reported to date. Racemic. (S)- and (R)-MDA were slightly less potent as releasing agents than (±)-, (+)- and (-)amphetamine respectively. (S)- and (R)-α-methyldopamine were the most potent releasing agents examined.