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Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
Published on: December 31, 2013
Monoterpenoid agonists of TRPV3
A K Vogt-Eisele1, K Weber, M A Sherkheli
1Department of Cell Physiology, Ruhr-University-Bochum, Bochum, Germany. Angela.Vogt-Eisele@rub.de
British Journal of Pharmacology
|April 11, 2007
Summary
Researchers identified potent monoterpene activators of the TRPV3 channel, a warmth-sensing protein in skin. A secondary hydroxyl group on the monoterpene structure is crucial for TRPV3 activation, offering insights into terpenoid pharmacology.
Area of Science:
- Molecular biology
- Neuroscience
- Pharmacology
Background:
- Transient receptor potential (TRP) V3 channels are thermosensitive ion channels primarily found in skin and neural tissues.
- TRPV3 is activated by warmth and camphor, and is implicated in skin sensitization.
- The related TRPM8 channel is activated by cool temperatures and compounds like (-)-menthol.
Purpose of the Study:
- To identify monoterpenoid compounds that activate TRPV3.
- To establish a structure-function relationship for TRPV3 activation by monoterpenoids.
- To investigate the overlap in receptor pharmacology between TRPV3 and TRPM8.
Main Methods:
- HEK293 cells and Xenopus laevis oocytes were used for experiments.
- Whole-cell patch clamp electrophysiology was employed to measure evoked currents.
- Dose-response curves were generated for potent TRPV3 agonists.
Main Results:
- Six monoterpenes, including carvacrol and thymol, were found to be significantly more potent TRPV3 activators than camphor.
- These potent activators possess EC(50) values up to 16 times lower than camphor.
- A key structural feature for potent activation is a ring-located hydroxyl group; these compounds minimally activated TRPM8.
Conclusions:
- Monoterpenes can activate TRPV3, suggesting a role for TRPV3 in mediating the effects of these compounds.
- A secondary hydroxyl group is a critical structural requirement for monoterpene-induced TRPV3 activation.
- This study elucidates the structure-activity relationship for TRPV3 agonists and expands understanding of terpenoid pharmacology.
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