Enantiomerically Pure Aminoindolizines: Bicyclic Ergoline Analogues with Dopamine Autoreceptor Activity
作者:Peter Gmeiner、Joachim Mierau、Georg Höfner
DOI:10.1002/ardp.19923250113
日期:——
stimulate selectively the prejunctional dopamine receptor has become a major challenge in recent years1,2), These autoreceptor agonists decrease synthesis and release of dopamine (OA), Thus, the symptoms of schizophrenia originated from dopamine hyperactivity in the mesolimbic system should be reduced. On the other hand, it has been shown that OA autoreceptor agonists fail to reveal classical OA antagonist
近年来,开发选择性刺激结前多巴胺受体的药物已成为一项重大挑战1,2),这些自身受体激动剂减少多巴胺 (OA) 的合成和释放,因此,精神分裂症的症状源于中脑边缘系统的多巴胺过度活跃应该减少。另一方面,已经表明,当给予动物时,OA 自身受体激动剂不能显示经典的 OA 拮抗剂副作用,如僵住症3)。由于假设高度敏感的 OA 自身受体类似于突触后 0-2 受体 4•5),我们计划通过对已知 0-2 激动剂的特定结构修饰来开发新型自身受体激动剂。一