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辛弗林:从痕量浓度到大量用于减肥。

Synephrine: from trace concentrations to massive consumption in weight-loss.

机构信息

REQUIMTE-Laboratório de Toxicologia, Departamento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.

出版信息

Food Chem Toxicol. 2011 Jan;49(1):8-16. doi: 10.1016/j.fct.2010.11.007. Epub 2010 Nov 12.

DOI:10.1016/j.fct.2010.11.007
PMID:21075161
Abstract

Synephrine is cited as 'the active component' of plants and dietary supplements used in weight loss. It became one of the most popular stimulants present in weight-loss products after the US Food and Drug Administration had interdicted the use of ephedrine-containing dietary supplements. Synephrine is also a trace amine that can be found in vertebrates and invertebrates. Synephrine acts on several adrenergic and serotonergic receptors and its activity on trace-amine-associated receptors has long been discussed. Synephrine exists in three different positional isomers; however, only p- and m-synephrine have been described in weight-loss products. The alleged effectiveness of synephrine-containing supplements is attributed to the thermogenic effects arising from synephrine's adrenergic stimulation. The growing use of synephrine has raised concerns since it has been accompanied by reports of adverse effects. Cardiac adverse events, including hypertension, tachyarrhythmia, variant angina, cardiac arrest, QT prolongation, ventricular fibrillation, myocardial infarction, and sudden death, have been the most common adverse effects associated with synephrine intake. The mechanisms involved in synephrine-induced cardiotoxicity are still unknown since studies related to its safety are scarce. This review will address general aspects concerning the pharmacology of synephrine, but will focus on the efficacy and toxicity aspects related to the use of synephrine in weight-loss.

摘要

辛弗林被称为植物和减肥膳食补充剂中的“活性成分”。在美国食品和药物管理局禁止使用含麻黄碱的膳食补充剂后,它成为减肥产品中最受欢迎的兴奋剂之一。辛弗林也是一种痕量胺,可在脊椎动物和无脊椎动物中发现。辛弗林作用于几种肾上腺素能和 5-羟色胺能受体,其对痕量胺相关受体的活性长期以来一直受到讨论。辛弗林存在三种不同的位置异构体;然而,只有 p-和 m-辛弗林在减肥产品中被描述过。含有辛弗林的补充剂据称是有效的,这归因于辛弗林的肾上腺素刺激引起的产热作用。由于伴随着不良反应的报告,辛弗林的使用越来越多,引起了人们的关注。与辛弗林摄入有关的最常见的不良反应包括高血压、心动过速性心律失常、变异性心绞痛、心脏骤停、QT 间期延长、心室颤动、心肌梗死和猝死。与辛弗林引起的心脏毒性相关的机制尚不清楚,因为与安全性相关的研究很少。这篇综述将讨论与辛弗林药理学相关的一般方面,但将重点介绍与减肥中使用辛弗林相关的疗效和毒性方面。

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