Craig J C, Torkelson S M, Findell P R, Weiner R I
Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco 94143.
J Med Chem. 1989 May;32(5):961-8. doi: 10.1021/jm00125a007.
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.
已经合成了一系列2-取代的八氢苯并[f]喹啉，并对其多巴胺激动剂活性进行了测定。在与放射性配体[3H]螺哌啶醇的竞争结合研究中，只有与多巴胺的β-旋转异构体构象相对应的化合物表现出双相活性。这些发现表明，具有β-旋转异构体构象的同系物所表现出的受体结合特征比相应的α-旋转异构体同系物更类似于麦角灵的受体结合特征。
