101. Modulation of CaV2.3 Calcium Channel Currents by Eugenol.
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Chung, G., Rhee, J. N., Jung, S. J., Kim, J. S., and Oh, S. B.
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EFFECT of drugs on calcium channels ,PATCH-clamp techniques (Electrophysiology) ,SODIUM channels ,CAPSAICIN ,ANALGESICS ,DENTAL research - Abstract
Eugenol, a natural congener of capsaicin, is a routine analgesic agent in dentistry. We have recently demonstrated the inhibition of Ca
V 2.2 calcium channel and sodium channel currents to be molecular mechanisms underlying the analgesic effect of eugenol. We hypothesized that CaV 2.3 channels are also modulated by eugenol and investigated its mode of action using the whole-cell patch-clamp technique in a heterologous expression system. Eugenol inhibited calcium currents in the E52 cell line, stably expressing the human CaV 2.3 calcium channels, where TRPV1 is not endogenously expressed. The extent of current inhibition was not significantly different between naïve E52 cells and TRPV1- expressing E52 cells, suggesting no involvement of TRPV1. In contrast, TRPV1 activation is prerequisite for the inhibition of CaV 2.3 calcium channels by capsaicin. The results indicate that eugenol has mechanisms distinct from those of capsaicin for modulating CaV 2.3 channels. We suggest that inhibition of CaV 2.3 channels by eugenol might contribute to its analgesic effect. [ABSTRACT FROM AUTHOR]- Published
- 2008
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