methamphetamine lethality in rats than 1, while it was as weak in inhibitory activity of apomorphine-induced stereotype in rats (ED50 greater than 500 mg/kg, p.o.) as 1. On the other hand, N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methyl-5-methylthio-2, 3-dihydrobenzofuran-7-carboxamide (30) showed a classical neuroleptic profile with a potency comparable to haloperidol in antagonistic activity on apomorphine-induced
合成了一系列具有稳定分子内氢键的
2,3-二氢苯并呋喃-7-羧酰胺,并在药理学模型中评估了其抗精神病活性。其中,N-[((1-丁基-2-
吡咯烷基)甲基] -2-甲基-5-
氨磺酰基-2,3-二氢
苯并呋喃-7-羧酰胺(15)显示出与sulpiride(1 )和比1更高的亲脂性。化合物15对
阿扑吗啡诱导的小鼠过度活动(ED50 = 30 mg / kg,口服)的拮抗活性比
对甲基苯丙胺致死力的增强作用强11倍,而对15如
阿斯吗啡对大鼠的刻板印象抑制作用弱(ED50大于500 mg / kg,口服)为1。另一方面,N-[(1-乙基-2-
吡咯烷基)甲基] -2-甲基- 5-甲
硫基-2,3-二氢
苯并呋喃-7-羧酰胺(30)在对
阿扑吗啡诱导的小鼠过度活动的拮抗活性方面表现出与
氟哌啶醇相当的经典
抗精神病药(ED50 = 0.65 mg / kg,口服)。还讨论了结构-活性关系。