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Comparison of the Effects of Pelargonic Acid Vanillylamide and Capsaicin on Human Vanilloid Receptors
Author(s) -
Weiser Thomas,
Roufogalis Basil,
Chrubasik Sigrun
Publication year - 2013
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.4817
Subject(s) - capsaicin , capsazepine , trpv1 , pungency , chemistry , pharmacology , receptor , antagonist , transient receptor potential channel , pepper , biochemistry , medicine , food science
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. Copyright © 2012 John Wiley & Sons, Ltd.