al-Rashood K A, Mustafa A A, Alhaider A A, Ginawi O T, Madani A A, el-Obeid H A
College of Pharmacy, Department of Pharmaceutical Chemistry, King Saud University, Riyadh, Saudi Arabia.
J Pharm Sci. 1988 Oct;77(10):898-901. doi: 10.1002/jps.2600771018.
A series of N-(4-phenyl- and 4-pyridyl-1-piperazinylethyl)- and N-(4-phenyl-1-piperidinylethyl)-phthalmides were synthesized and tested for antipsychotic activity. All compounds suppressed the spontaneous motor activity and the apomorphine-induced climbing in mice and pergolide-induced locomotor activity in rats, demonstrating psychotropic properties equal to the corresponding properties of sulpiride. Although the compounds, like sulpiride, were less potent than haloperidol in blocking the locomotor activities, they caused no catalepsy, a major side effect following treatment with conventional antipsychotic agents. It is likely that the new compounds produce their neuroleptic activities through inhibition of limbic dopamine receptors.
合成了一系列N-（4-苯基和4-吡啶基-1-哌嗪基乙基）-和N-（4-苯基-1-哌啶基乙基）-邻苯二甲酰胺，并对其抗精神病活性进行了测试。所有化合物均能抑制小鼠的自发运动活性以及阿扑吗啡诱导的攀爬行为，以及大鼠中培高利特诱导的运动活性，显示出与舒必利相应特性相当的精神otropic特性。尽管这些化合物与舒必利一样，在阻断运动活性方面比氟哌啶醇的效力低，但它们不会引起僵住症，这是传统抗精神病药物治疗后的主要副作用。新化合物很可能通过抑制边缘多巴胺受体产生其抗精神病活性。
