Ogren S O, Hall H, Köhler C, Magnusson O, Florvall L
Arzneimittelforschung. 1985;35(8):1227-31.
The pharmacology of S-(-)-3-bromo-2, 6-dimethoxy-N-(1-ethyl-2-pyrrolidinylone-ethyl)-benzamide (remoxipride), a new neuroleptic compound belonging to the benzamide group, has been thoroughly investigated using a number of different techniques. The compound blocks apomorphine-induced stereotypies and hyperactivity, indicating potent antidopaminergic activity. However, in contrast to many other antidopaminergic compounds, remoxipride induces only weak and atypical catalepsy, which indicates that remoxipride might exert less antidopaminergic side effects than other neuroleptic drugs. In vivo receptor binding studies using 3H-spiperone show that remoxipride preferentially blocks dopamine receptors only are blocked to 60% even at very high doses. In vitro receptor binding studies show that remoxipride is devoid of affinity for receptors other than the dopamine D2 receptors except at higher concentrations. These results indicate that remoxipride should be a clinically effective neuroleptic compound exerting less extrapyramidal side effects than the neuroleptics currently used.
S-(-)-3-溴-2,6-二甲氧基-N-(1-乙基-2-吡咯烷酮基乙基)-苯甲酰胺(瑞莫必利)是一种属于苯甲酰胺类的新型抗精神病化合物,已使用多种不同技术对其药理学进行了深入研究。该化合物可阻断阿扑吗啡诱导的刻板行为和多动,表明具有强效抗多巴胺能活性。然而,与许多其他抗多巴胺能化合物不同,瑞莫必利仅诱导轻微且非典型的僵住症,这表明瑞莫必利可能比其他抗精神病药物产生更少的抗多巴胺能副作用。使用3H-螺哌隆进行的体内受体结合研究表明,瑞莫必利优先阻断多巴胺受体,即使在非常高的剂量下,其他受体也仅被阻断60%。体外受体结合研究表明,除了在较高浓度下,瑞莫必利对多巴胺D2受体以外的受体没有亲和力。这些结果表明,瑞莫必利应该是一种临床有效的抗精神病化合物,其锥体外系副作用比目前使用的抗精神病药物更少。