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The Scientific World Journal
Volume 2014 (2014), Article ID 184526, 6 pages
Research Article

Pharmacodynamics of TRPV1 Agonists in a Bioassay Using Human PC-3 Cells

1Laboratori de Fisiologia Digestiva, Departament de Cirurgia, Hospital de Mataró, Universitat Autònoma de Barcelona, 08304 Mataró, Spain
2Centro de Investigación Biomédica en Red de Enfermedades Hepáticas y Digestivas, 28029 Madrid, Spain
3Departament de Biologia Cel·lular, Fisiologia i Immunologia, Universitat Autònoma de Barcelona (UAB), 08193 Bellaterra, Spain

Received 19 August 2013; Accepted 5 December 2013; Published 2 February 2014

Academic Editors: J.-T. Cheng and E. Hopper-Borge

Copyright © 2014 Daniel Alvarez-Berdugo et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Purpose. TRPV1 is a multimodal channel mainly expressed in sensory neurons. We aimed to explore the pharmacodynamics of the TRPV1 agonists, capsaicin, natural capsaicinoids, and piperine in an in vitro bioassay using human PC-3 cells and to examine desensitization and the effect of the specific antagonist SB366791. Methods. PC-3 cells expressing TRPV1 were incubated with Fluo-4. Fluorescence emission changes following exposition to agonists with and without preincubation with antagonists were assessed and referred to maximal fluorescence following the addition of ionomycin. Concentration-response curves were fitted to the Hill equation. Results. Capsaicin and piperine had similar pharmacodynamics ( 204.8 ± 184.3% piperine versus 176.6 ± 35.83% capsaicin, , Hill coefficient 0.70 ± 0.50 piperine versus 1.59 ± 0.86 capsaicin, ). In contrast, capsaicinoids had lower (40.99 ± 6.14% capsaicinoids versus 176.6 ± 35.83% capsaicin, ). All the TRPV1 agonists showed significant desensitization after the second exposition and their effects were strongly inhibited by SB366791. Conclusion. TRPV1 receptor is successfully stimulated by capsaicin, piperine, and natural capsaicinoids. These agonists present desensitization and their effect is significantly reduced by a TRPV1-specific antagonist. In addition, PC-3 cell bioassays proved useful in the study of TRPV1 pharmacodynamics.