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Activation of Vanilloid Receptor 1 (VR1) by Eugenol

B.H. Yang*, Z.G. Piao*, Y.-B. Kim, C.-H. Lee, J.K. Lee, K. Park, J.S. Kim, and S.B. Oh#

Department of Physiology, College of Dentistry and Dental Research Institute, Seoul National University, 28-2 Yeongeon-Dong ChongNo-Ku, Seoul, Korea 110-749;



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Figure 1. Eugenol activated inward currents in VR1-expressing HEK 293 cells. (A) The current profiles induced by the application of eugenol (1 mM) and capsaicin (1 µM). The holding potential was -60 mV. (B) The inward current activated by eugenol was completely inhibited by RR (10 µM) and CZP (10 µM). Since the eugenol-activated currents by the first and second applications were not significantly different (top trace), the eugenol-activated currents were compared after cells were pre-treated with either RR for 1.5 min prior to the second application of eugenol and RR (middle trace) or CZP for 1.5 min prior to the second application of eugenol and CPZ (bottom trace).

 


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Figure 2. Effects of eugenol on [Ca2+]i in VR1-expressing HEK 293 cells. (A) Eugenol (1 mM) increased [Ca2+]i in a capsaicin-responsive cell. Carbachol (CCh, 10 µM), as a positive control, evoked Ca transient through muscarinic receptors endogenously expressed on the cells. The eugenol-induced Ca transient was abolished by CZP (10 µM) (B) and RR (10 µM) (C).

 


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Figure 3. Eugenol evoked inward currents in capsaicin-responsive TG neurons. (A) Eugenol (1 mM) and capsaicin (1 µM) activated inward currents in the same cells. Eugenol-induced inward currents were blocked by RR (10 µM) (B) and CZP (10 µM) (C). Due to the difference of current amplitude, the current traces in C were displayed separately although measured in the same cell.

 


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Figure 4. Effects of eugenol on [Ca2+]i in capsaicin-responsive TG neurons. (A) Eugenol (1 mM) increased [Ca2+]i. The enhancement of [Ca2+]i was abolished by CZP (10 µM) (B) and RR (C). Capsaicin (1 µM), as a positive control, also evoked Ca transient (A), which was completely abolished by CZP (10 µM) (B) and RR (10 µM) (C).

 





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