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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Serotonin releasing agents. Neurochemical, therapeutic and adverse effects.
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Serotonin releasing agents. Neurochemical, therapeutic and adverse effects.

机译：血清素释放剂。神经化学，治疗和不良反应。

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This review summarizes the neurochemical, therapeutic and adverse effects of serotonin (5-HT) releasing agents. The 5-HT releaser (plus minus)-fenfluramine is composed of two stereoisomers, (+)-fenfluramine and (minus sign)-fenfluramine, which are N-de-ethylated to yield the metabolites, (+)-norfenfluramine and (minus sign)-norfenfluramine. Fenfluramines and norfenfluramines are 5-HT transporter substrates and potent 5-HT releasers. Other 5-HT releasing agents include m-chlorophenylpiperazine (mCPP), a major metabolite of the antidepressant drug trazodone. Findings from in vitro and in vivo studies support the hypothesis that fenfluramines and mCPP release neuronal 5-HT via a non-exocytotic carrier-mediated exchange mechanism involving 5-HT transporters. (+)-Norfenfluramine is a potent 5-HT(2B) and 5-HT(2C) receptor agonist. The former activity may increase the risk of developing valvular heart disease (VHD), whereas the latter activity is implicated in the anorectic effect of systemic fenfluramine. Anorectic agents that increase the risk of developing primary pulmonary hypertension (PPH) share the common property of being 5-HT transporter substrates. However, these drugs vary considerably in their propensity to increase the risk of PPH. In this regard, neither trazodone nor mCPP is associated with PPH. Similarly, although some 5-HT substrates can deplete brain 5-HT (fenfluramine), others do not (mCPP). In addition to the established indication of obesity, 5-HT releasers may be helpful in treating psychiatric problems such as drug and alcohol dependence, depression and premenstrual syndrome. Viewed collectively, it seems possible to develop new medications that selectively release 5-HT without the adverse effects of PPH, VHD or neurotoxicity. Such agents may have utility in treating a variety of psychiatric disorders.
机译：这篇综述总结了5-羟色胺（5-HT）释放剂的神经化学，治疗和不良作用。 5-HT释放剂（+负）-氟氟拉明由两个立体异构体（+）-氟氟拉明和（-负号）-氟氟拉明组成，它们经过N-去乙基化以生成代谢物（+）-去氟氟拉明和（-标志）-去甲氟拉明。芬氟拉明和去甲氟拉明是5-HT转运蛋白的底物和有效的5-HT释放剂。其他5-HT释放剂包括间氯苯基哌嗪（mCPP），这是抗抑郁药曲唑酮的主要代谢产物。体外和体内研究的结果支持以下假设：芬氟拉明和mCPP通过涉及5-HT转运蛋白的非胞吐载体介导的交换机制释放神经元5-HT。 （+）-Norfenfluramine是有效的5-HT（2B）和5-HT（2C）受体激动剂。前者的活动可能会增加患瓣膜性心脏病（VHD）的风险，而后者的活动则与全身性芬氟拉明的厌食作用有关。厌食药会增加患原发性肺动脉高压（PPH）的风险，它们具有5-HT转运底物的共同特性。但是，这些药物增加PPH风险的倾向差异很大。在这方面，曲唑酮和mCPP都不与PPH相关。同样，尽管某些5-HT底物可以消耗大脑5-HT（芬氟拉明），但其他一些则不能（mCPP）。除了确定的肥胖症迹象外，5-HT释放剂还可能有助于治疗精神疾病，例如药物和酒精依赖，抑郁症和经前综合症。总体上看，似乎有可能开发出选择性释放5-HT而不会产生PPH，VHD或神经毒性的药物。此类试剂可用于治疗多种精神疾病。

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