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5-HT2 配体在焦虑和抑郁治疗中的应用。

5-HT2 ligands in the treatment of anxiety and depression.

机构信息

EA3544 University Paris-XI, Laboratoire de Neuropharmacologie, Fac. Pharmacie, F-92296, Châtenay-Malabry cedex, France.

出版信息

Expert Opin Investig Drugs. 2012 Nov;21(11):1701-25. doi: 10.1517/13543784.2012.719872. Epub 2012 Aug 24.

Abstract

INTRODUCTION

One third of depressed patients do not respond adequately to conventional antidepressants including the selective serotonin reuptake inhibitors (SSRIs). Therefore, multi-target drugs or augmentation strategies have been developed for the management of SSRIs-resistant patients. In this context, the 5-HT(2) receptor subtypes represent promising targets but their precise roles have yet to be determined.

AREAS COVERED

The aim of this review is to shed some light on the preclinical evidence supporting the use of 5-HT(2A) and/or 5-HT(2C) receptor antagonists such as antipsychotics, as potential effective adjuncts in SSRIs-resistant depression. This review synthesizes the current literature about the behavioral, electrophysiological and neurochemical effects of 5-HT(2) receptors ligands on the monoaminergic systems but also on adult hippocampal neurogenesis.

EXPERT OPINION

Although studies support the hypothesis that the inactivation of 5-HT(2A) and/or 5-HT(2C) receptors might be of interest to reinforce different facets of the therapeutic activity of SSRIs, this pharmacological strategy remains debatable notably because of the lack of chronic data in relevant animal models. Conversely, emerging evidence suggests that the activation of 5-HT(2B) receptor is required for antidepressant-like activity, opening the way to new therapeutic approaches. However, the potential risks related to the enhancement of monoaminergic neurotransmissions could represent a major concern.

摘要

简介

三分之一的抑郁症患者对包括选择性 5-羟色胺再摄取抑制剂(SSRIs)在内的传统抗抑郁药反应不足。因此,已经开发了多靶标药物或增强策略来治疗 SSRIs 耐药患者。在这种情况下,5-HT(2)受体亚型是很有前途的靶点,但它们的确切作用仍有待确定。

涵盖领域

本文旨在阐明支持使用 5-HT(2A)和/或 5-HT(2C)受体拮抗剂(如抗精神病药)作为 SSRIs 耐药性抑郁症潜在有效辅助药物的临床前证据。本文综合了目前关于 5-HT(2)受体配体对单胺能系统以及成年海马神经发生的行为、电生理和神经化学影响的文献。

专家意见

尽管研究支持这样一种假设,即失活 5-HT(2A)和/或 5-HT(2C)受体可能有助于增强 SSRIs 的治疗作用的不同方面,但这种药理策略仍然存在争议,特别是因为缺乏相关动物模型的慢性数据。相反,新出现的证据表明,5-HT(2B)受体的激活对于抗抑郁样活性是必需的,为新的治疗方法开辟了道路。然而,增强单胺能神经传递可能带来的潜在风险是一个主要关注点。

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