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Pharmacodynamics of TRPV1 Agonists in a Bioassay Using Human PC-3 Cells
Joint Authors
Alvarez-Berdugo, Daniel
Jiménez, Marcel
Clavé, Pere
Rofes, Laia
Source
Issue
Vol. 2014, Issue 2014 (31 Dec. 2014), pp.1-6, 6 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2014-02-02
Country of Publication
Egypt
No. of Pages
6
Main Subjects
Medicine
Information Technology and Computer Science
Abstract EN
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 ( E max 204.8 ± 184.3% piperine versus 176.6 ± 35.83% capsaicin, P = 0.8814 , Hill coefficient 0.70 ± 0.50 piperine versus 1.59 ± 0.86 capsaicin, P = 0.3752 ).
In contrast, capsaicinoids had lower E max (40.99 ± 6.14% capsaicinoids versus 176.6 ± 35.83% capsaicin, P < 0.001 ).
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.
American Psychological Association (APA)
Alvarez-Berdugo, Daniel& Jiménez, Marcel& Clavé, Pere& Rofes, Laia. 2014. Pharmacodynamics of TRPV1 Agonists in a Bioassay Using Human PC-3 Cells. The Scientific World Journal،Vol. 2014, no. 2014, pp.1-6.
https://search.emarefa.net/detail/BIM-1048643
Modern Language Association (MLA)
Alvarez-Berdugo, Daniel…[et al.]. Pharmacodynamics of TRPV1 Agonists in a Bioassay Using Human PC-3 Cells. The Scientific World Journal No. 2014 (2014), pp.1-6.
https://search.emarefa.net/detail/BIM-1048643
American Medical Association (AMA)
Alvarez-Berdugo, Daniel& Jiménez, Marcel& Clavé, Pere& Rofes, Laia. Pharmacodynamics of TRPV1 Agonists in a Bioassay Using Human PC-3 Cells. The Scientific World Journal. 2014. Vol. 2014, no. 2014, pp.1-6.
https://search.emarefa.net/detail/BIM-1048643
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1048643