PDF(Pubmed)
Abstract：
Pre-workout supplements are popular among sport athletes and overweight individuals. Phenethylamines (PEAs) and alkylamines (AA) are widely present in these supplements. Although the health effects of these analogues are not well understood yet, they are hypothesised to be agonists of adrenergic (ADR) and trace amine-associated receptors (TAARs). Therefore, we aimed to pharmacologically characterise these compounds by investigating their activating properties of ADRs and TAAR1 in vitro. The potency and efficacy of the selected PEAs and AAs was studied by using cell lines overexpressing human ADRα1A/α1B/α1D/α2a/α2B/β1/β2 or TAAR1. Concentration-response relationships are expressed as percentages of the maximal signal obtained by the full ADR agonist adrenaline or the full TAAR1 agonist phenethylamine. Multiple PEAs activated ADRs (EC50 = 34 nM-690 µM; Emax = 8-105%). Almost all PEAs activated TAAR1 (EC50 = 1.8-92 µM; Emax = 40-104%). Our results reveal the pharmacological profile of PEAs and AAs that are often used in food supplements. Several PEAs have strong agonistic properties on multiple receptors and resemble potencies of the endogenous ligands, indicating that they might further stimulate the already activated sympathetic nervous system in exercising athletes via multiple mechanisms. The use of supplements containing one, or a combination of, PEA(s) may pose a health risk for their consumers.
摘要：
锻炼前补充剂在运动运动员和超重者中很受欢迎。苯乙胺(PEA)和烷基胺(AA)广泛存在于这些补充剂中。虽然这些类似物对健康的影响还没有很好的理解，假设它们是肾上腺素能(ADR)和痕量胺相关受体(TAARs)的激动剂.因此,我们旨在通过研究ADR和TAAR1的体外激活特性来对这些化合物进行药理学表征。通过使用过表达人ADRα1A/α1B/α1D/α2a/α2B/β1/β2或TAAR1的细胞系研究了所选PEA和AA的效力和功效。浓度-反应关系表示为由完全ADR激动剂肾上腺素或完全TAAR1激动剂苯乙胺获得的最大信号的百分比。多种PEAs激活的ADR（EC50=34nM-690µM；Emax=8-105%）。几乎所有PEAs都激活了TAAR1（EC50=1.8-92µM；Emax=40-104％）。我们的结果揭示了经常用于食品补充剂的PEAs和AA的药理学特征。几种PEAs对多种受体具有强烈的激动特性，并且类似于内源性配体的效力，这表明它们可能通过多种机制进一步刺激运动员锻炼时已经激活的交感神经系统。使用含有一种的补充剂，或组合，PEA可能对其消费者构成健康风险。
