New life sciences data have been reported by S.P. Lee and co-authors

Tag : Alkyl Phenols

2008 JUN 6 - ( NewsRx.com ) -- Research findings, 'Thymol and related alkyl phenols activatethe hTRPA1 channel,' are discussed in a new report (see also Life Sciences ). According to a study from the United States, "Thymol, a majorcomponent of thyme and oregano, has medical uses in oral careproducts as an astringent and antibiotic. Its distinctive sharpodour and pungent flavour are considered aversive properties."
"The molecular basis of these aversive properties is not wellunderstood. EXPERIMENTAL APPROACH: The ability of thymol toactivate human transient receptor potential channel A1 (hTRPA1)expressed in stably transfected human embryonic kidney 293 (HEK293)cells was measured by membrane potential and calcium-sensitive dyesin a fluorescence-imaging plate reader (FLIPR) assay. Directactivation of hTRPA1 currents was measured by whole-cell voltageclamp recording. Intracellular calcium changes were measured usingfura-2 dye. The FLIPR assay was also used to measure membranepotential changes elicited by thymol after pretreatment withcamphor, a known TRPA1 inhibitor. The ability of related alkylphenols to activate hTRPA1 was also determined. Thymol potentlyactivated a membrane potential response and intracellular calciumincrease in hTRPA1-expressing HEK293 cells in aconcentration-dependent manner. Activation by thymol desensitizedhTRPA1 to further exposure to thymol or the known ligand allylisothiocyanate (AITC). The related phenols2-tert-butyl-5-methylphenol, 2,6-diisopropylphenol (propofol) andcarvacrol also activated hTRPA1. Phenols with less bulky carbonsubstitutions and lower logP values were less potent in general,"wrote S.P. Lee and colleagues, .
The researchers concluded: "The response to thymol was blocked bycamphor.AND IMPLICATIONS: These results suggest a role for hTRPA1activation in the reported pungent and aversive properties of someof these pharmaceutically important phenols."
Lee and colleagues published their study in British Journal of Pharmacology (Thymol and related alkyl phenols activate the hTRPA1 channel. British Journal of Pharmacology , 2008;153(8):1739-49).
For more information, contact S.P. Lee, Discovery Research,Redpoint Bio Corporation, Ewing, NJ USA..
Publisher contact information for the British Journal of Pharmacology is: Nature Publishing Group, Macmillan Building, 4 Crinan St.,London N1 9XW, England.
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