Costall B, Domeney A M, Gerrard P A, Kelly M E, Naylor R J
Postgraduate School of Studies in Pharmacology, University of Bradford, UK.
J Pharm Pharmacol. 1988 Apr;40(4):302-5. doi: 10.1111/j.2042-7158.1988.tb05254.x.
Zacopride, a substituted benzamide derivative, was compared with diazepam in three models of experimental or provoked anxiety. The drug's action (i) in reducing aversion to a brightly lit environment was assessed in mice using a two compartment black and white test box system, (ii) in disinhibiting a suppressed behaviour was measured in the rat social interaction test under high light/unfamiliar conditions and (iii) in antagonizing a defensive response in the marmoset was assessed using the threat of a human presence. Both zacopride and diazepam enhanced exploratory behaviour and social interaction in the mouse and rat models and antagonized the defensive response in the marmoset, zacopride being 100 times more potent than diazepam. It is concluded that the 5-HT3 receptor antagonist, zacopride, alters rodent and primate behaviour in a manner consistent with that of an anxiolytic agent.
扎考必利是一种取代苯甲酰胺衍生物，在三种实验性或诱发性焦虑模型中与地西泮进行了比较。该药物的作用：（i）在使用两室黑白测试箱系统的小鼠中评估其减少对明亮环境厌恶的作用；（ii）在高光/不熟悉条件下的大鼠社交互动测试中测量其解除被抑制行为的作用；（iii）在狨猴中使用人类出现的威胁评估其对抗防御反应的作用。扎考必利和地西泮均增强了小鼠和大鼠模型中的探索行为和社交互动，并对抗了狨猴的防御反应，扎考必利的效力比地西泮强100倍。得出的结论是，5-羟色胺3受体拮抗剂扎考必利以与抗焦虑药一致的方式改变啮齿动物和灵长类动物的行为。
