Boehringer Ingelheim Pharma GmbH & Co. KG, Ingelheim am Rhein, Germany.
Phytother Res. 2013 Jul;27(7):1048-53. doi: 10.1002/ptr.4817. Epub 2012 Sep 7.
Pelargonic acid vanillylamide is like capsaicin a natural capsaicinoid from chili peppers and commonly used in food additives to create a hot sensation, even in self-defense pepper sprays and as an alternative to capsaicin in medical products for topical treatment of pain. Although the chemical structures of both compounds are similar, preclinical data suggest that capsaicin is the more potent compound. We therefore performed voltage-clamp recordings using cells transfected with the human vanilloid receptor TRPV1 in order to assess the responses of pelargonic acid vanillylamide and capsaicin at the receptor level. We provide evidence that at the molecular target TRPV1, the concentration-response curves, kinetics of current activation, as well as inhibition by the competitive antagonist capsazepine were not significantly different between the two capsaicinoids. We suggest that the different effects of the two capsaicinoids observed in previous studies may rather be due to different physicochemical or pharmacokinetic properties than to different pharmacological profiles at the receptor level.
壬酸香草酰胺类似于辣椒素，是辣椒中的一种天然辣椒素，常用于食品添加剂中，以产生辣味，甚至用于自卫性胡椒喷雾，以及作为医疗产品中治疗疼痛的辣椒素替代品，用于局部治疗。尽管这两种化合物的化学结构相似，但临床前数据表明辣椒素是更有效的化合物。因此，我们使用转染人香草素受体 TRPV1 的细胞进行电压钳记录，以评估壬酸香草酰胺和辣椒素在受体水平的反应。我们提供的证据表明，在分子靶标 TRPV1 上，两种辣椒素的浓度-反应曲线、电流激活动力学以及竞争性拮抗剂辣椒素的抑制作用没有显著差异。我们认为，在以前的研究中观察到的两种辣椒素的不同作用可能更多地归因于不同的物理化学或药代动力学特性，而不是受体水平上的不同药理学特征。
