Synthesis and dopaminergic activity of 2-substituted octahydrobenzo[f]quinolines.
Synthesis and dopaminergic activity of 2-substituted octahydrobenzo[f]quinolines.
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DOI：
10.1021/jm00125a007
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发表时间：
1989-05
影响因子：
7.3
通讯作者：
J. Craig;S. Torkelson;P. Findell;R. Weiner
中科院分区：
文献类型：
--
作者：
J. Craig;S. Torkelson;P. Findell;R. Weiner
合成了一系列2-取代八氢苯并[f]喹啉类化合物，并测定了它们的多巴胺激动活性。只有对应于多巴胺的β-旋转异构体构象的化合物在与放射性配体[3 H]spiroperidol的竞争结合研究中显示出双相活性。这些研究结果表明，具有β-旋转异构体构象的同系物显示受体结合特征，类似于麦角林的受体结合特征比相应的α-旋转异构体同系物更接近。
A series of 2-substituted octahydrobenzo[f]quinolines has been synthesized and assayed for dopamine agonist activity. Only the compounds corresponding to the beta-rotameric conformation of dopamine showed biphasic activity in competition binding studies with the radioligand [3H]spiroperidol. These findings suggest that the congeners possessing the beta-rotamer conformation show receptor-binding characteristics that resemble those of the ergolines more closely than do those of the corresponding alpha-rotamer congeners.