Pharmacy Group, Birla Institute of Technology & Science, Rajasthan, India.
J Psychopharmacol. 2010 Apr;24(4):455-69. doi: 10.1177/0269881109348161. Epub 2010 Feb 1.
The serotonergic mechanisms have been successfully utilized by the majority of antidepressant drug discovery programmes, while the search for newer targets remains persistent. The present review focused on the serotonin type-3 receptor, the only ion channel subtype in the serotonin family. Behavioural, neurochemical, electrophysiological and molecular analyses, including the results from our laboratory, provided substantial evidence that rationalizes the correlation between serotonin type-3 receptor modulation and rodent depressive-like behaviour. Nevertheless, the reports on polymorphism of serotonin type-3 receptor genes and data from clinical studies (on serotonin type-3 receptor antagonists) were insufficient to corroborate the involvement of this receptor in the neurobiology of depression. The preclinical and clinical studies that have contradicted the antidepressant-like effects of serotonin type-3 receptor antagonists and the reasons underlying such disagreement were discussed. Finally, this critical review commended the serotonin type-3 receptor as a candidate neuronal antidepressant drug target.
大多数抗抑郁药物研发项目都成功利用了血清素能机制,而寻找新的靶点仍然是一个持续的目标。本综述集中于血清素 3 型受体,这是血清素家族中唯一的离子通道亚型。行为、神经化学、电生理学和分子分析,包括我们实验室的结果,提供了大量的证据,合理地解释了血清素 3 型受体调节与啮齿类动物抑郁样行为之间的相关性。然而,关于血清素 3 型受体基因多态性的报道和来自临床研究(关于血清素 3 型受体拮抗剂)的数据,不足以证实该受体参与抑郁症的神经生物学。本文讨论了与血清素 3 型受体拮抗剂的抗抑郁作用相矛盾的临床前和临床研究,以及导致这种分歧的原因。最后,这篇批判性综述称赞血清素 3 型受体是候选的神经元抗抑郁药物靶点。