Costall B, Naylor R J
School of Pharmacy, University of Bradford, West Yorkshire, United Kingdom.
Pharmacol Toxicol. 1992 Dec;71(6):401-15. doi: 10.1111/j.1600-0773.1992.tb00570.x.
5-HT3 receptors have an exclusive neuronal location and evidence is presented of their involvement in behaviour. 5-HT3 receptor antagonists such as ondansetron, tropisetron and zacopride have provided the critical pharmacological tools to reveal a potent and efficacious ability to regulate disturbed behaviour. Thus the 5-HT3 receptor antagonists will restore to normal rodent and primate behaviour disturbed by increasing limbic dopamine function, aversive situations, cognitive impairments and drug abuse. The remarkable feature of their action is a failure to modify normal behaviour. This unique pharmacological signature has ensured a wide interest in the potential role of the 5-HT3 receptor antagonists in the treatment of schizophrenia, anxiety, age related memory impairment and the problems of withdrawal from drugs of abuse. The preclinical data and preliminary clinical observations are presented.
5-羟色胺3受体仅存在于神经元中，并且有证据表明它们参与了行为活动。昂丹司琼、托烷司琼和扎考必利等5-羟色胺3受体拮抗剂提供了关键的药理学工具，以揭示其调节紊乱行为的强大而有效的能力。因此，5-羟色胺3受体拮抗剂能使因边缘多巴胺功能增强、厌恶情境、认知障碍和药物滥用而紊乱的啮齿动物和灵长类动物行为恢复正常。它们作用的显著特点是不会改变正常行为。这种独特的药理学特征使得人们对5-羟色胺3受体拮抗剂在治疗精神分裂症、焦虑症、与年龄相关的记忆障碍以及药物滥用戒断问题中的潜在作用产生了广泛兴趣。本文展示了临床前数据和初步临床观察结果。
