Molecular Mechanisms of TRPV1 Channel Activation

Andrés Jara-Oseguera1, Andrés Nieto-Posadas2, Arpad Szallasi3, 4, León D. Islas1, Tamara Rosenbaum*, 2
1 Departamento de Fisiología, Facultad de Medicina, Universidad Nacional Autónoma de México, D.F. 04510 México
2 Departamento de Neurodesarrollo y Fisiología, División Neurociencias, Instituto de Fisiología, Celular, Universidad Nacional Autónoma de México, D.F. 04510, México
3 Department of Pathology, Monmouth Medical Center, Long Branch, NJ 07740, USA
4 Department of Pathology, Drexel University College of Medicine, Philadelphia, PA 19102, USA

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© 2010 Jara-Oseguera et al.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

* Address correspondence to this author at the Departamento de Neurodesarrolloy Fisiología, División Neurociencias, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, D.F. 04510, México; Tel: +5255 5622 56 24; Fax: +52 55 5622 56 07; E-mail:


Transient Receptor Potential (TRP) cation channels participate in various fundamental processes in cell- andorganism-physiology in unicellular eukaryotes, invertebrates and vertebrates. Interestingly, many TRP channels function as detectors of sensory stimuli. The TRPV1 (vanilloid 1) channel serves as an integrator of noxious chemical and physical stimuli known to cause irritation and pain, such as elevated temperatures, acids, and irritant chemical compounds, and its activation has been linked to acute nociceptive pain and neurogenic inflammation. The mechanisms by which the channel detects incoming stimuli, how the sensing domains are coupled to channel gating and how these processes are connected to specific structural regions in the channel are not fully understood, but valuable information is available. Many sites involved in agonist detection have been characterized and gating models that describe many features of the channel’s behavior have been put forward. Structural and functional information indicates TRP channels are similar to voltage-activated potassium channels, with a tetrameric organization and six-transmembrane-region subunits, a pore domain with multi-ion binding properties and an intracellular S6 gate that seems to be the point of convergence of the many activation modalities leading to the opening of the ion conduction pathway. Furthermore, TRPV1 expression is altered in various disease states and TRPV1 gene polymorphism was speculated to play a role in pain sensation. The complex activation and regulation of TRPV1 may have important implications for drug development

Keywords: Ion Channels, Activation Gate, TRPV1, Pain, Capsaicin.