Division of Pharmacology, Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cathays Park, Cardiff CF10 3NB, UK.
Pharmacol Ther. 2010 Mar;125(3):363-75. doi: 10.1016/j.pharmthera.2009.11.005. Epub 2009 Dec 4.
Trace amines, including tyramine, beta-phenylethylamine (beta-PEA), tryptamine and octopamine, are biologically active amines mostly based on phenylethylamine, occurring in the body in trace amounts. They are a diverse group of naturally occurring and synthetic amines, which are also found in the diet and in herbal plants, such as ephedrine and cathinone. They include amphetamine and its analogues, such as MDMA ('ecstasy'), and synthetic proprietary sympathomimetic agents such as phenylpropanolamine and pseudoephedrine. On the vascular system they cause vasoconstriction and a rise in blood pressure. This effect is the basis of their use as nasal decongestants. For over 50 years, they have been assumed to be indirectly acting sympathomimetic amines, their responses being due to the release of noradrenaline from sympathetic neurones. There are, however, results that suggest that this is not their only mechanism of action and that they may also exert direct vascular effects independent of a noradrenergic mechanism. Recently, a group of novel trace amine-associated receptors (TAARs) have been cloned and identified in the brain and peripheral tissues including blood vessels. Trace amines bind to these cloned receptors and it is suggested that their vasoconstrictor effects can in part be attributed to this mechanism. This review describes the cardiovascular pharmacology of this diverse group of amines, their structures and uses and their endogenous synthesis and metabolism. The review also considers their clinical relevance as constituents of the diet, as therapeutic agents (ritodrine, phenylpropanolamine, and pseudoephedrine) and as drugs of abuse (amphetamine, 'ecstasy') and their mechanisms of action.
痕量胺，包括酪胺、β-苯乙胺（β-PEA）、色胺和章鱼胺，是生物活性胺，主要基于苯乙胺，在体内以痕量存在。它们是一组多样化的天然和合成胺，也存在于饮食和草药植物中，如麻黄碱和卡西酮。它们包括安非他命及其类似物，如摇头丸（“摇头丸”），以及合成专有拟交感胺，如苯丙醇胺和伪麻黄碱。在血管系统中，它们会导致血管收缩和血压升高。这种作用是它们作为鼻减充血剂的基础。五十多年来，人们一直认为它们是间接作用的拟交感胺，它们的作用是由于去甲肾上腺素从交感神经元释放。然而，有结果表明，这不是它们唯一的作用机制，它们也可能发挥独立于去甲肾上腺素机制的直接血管作用。最近，一组新型痕量胺相关受体（TAARs）已在大脑和外周组织（包括血管）中被克隆和鉴定。痕量胺与这些克隆受体结合，其血管收缩作用部分归因于这种机制。这篇综述描述了这组多样化胺的心血管药理学，包括它们的结构和用途、内源性合成和代谢。综述还考虑了它们作为饮食成分、治疗剂（利托君、苯丙醇胺和伪麻黄碱）和滥用药物（安非他命、“摇头丸”）的临床相关性，以及它们的作用机制。
