• integral to plasma membrane • membrane • integral to membrane
Biological Process:
• thermoregulation • ion transport • calcium ion transport • cell surface receptor linked signal transduction • chemosensory behavior • response to pH • response to heat • sensory perception of pain • thermoception
The Transient receptor potential vanilloid 1 or TRPV1 can refer to the TPR cation channel receptor or the gene which encodes it in Homo sapiens.
TRPV1 is a nonselective ligand-gated cation channel that may be activated by a wide variety of exogenous and endogenous stimuli, including heat greater than 43°C, low pH, anandamide, N-arachidonoyl-dopamine, and capsaicin. TRPV1 receptors are found in the central nervous system and the peripheral nervous system and are involved in the transmission and modulation of pain, as well as the integration of diverse painful stimuli. [1].[2]
Novel TRPV1 antagonists have shown efficacy in reducing nociception from inflammatory and neuropathic pain models in rats. This provides evidence that TRPV1 is the capsaicin's sole receptor.[3]
In humans, drugs acting at TRPV1 receptors could potentially be used to treat neuropathic pain associated with multiple sclerosis, chemotherapy, or amputation, as well as pain associated with the inflammatory response of damaged tissue, such as in osteoarthritis.
^ Cui et al. TRPV1 Receptors in the CNS Play a Key Role in Broad-spectrum Analgesia of TRPV1 Antagonists. The Journal of Neuroscience 26(37), 9385-93 (2006) PMID 16971522
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Huang SM, Bisogno T, Trevisani M, Al-Hayani A, De Petrocellis L, Fezza F, Tognetto M, Petros TJ, Krey JF, Chu CJ, Miller JD, Davies SN, Geppetti P, Walker JM, Di Marzo V (2007). "An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors.". Proceedings of the national academy of sciences99 (12): 8400-5. PMID 12060783.
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Story GM, Crus-Orengo L (July-August 2007). "Feel the burn". American Scientist95 (4): 326-333. ISSN 0003-0996.
Further reading
Heiner I, Eisfeld J, Lückhoff A (2004). "Role and regulation of TRP channels in neutrophil granulocytes.". Cell Calcium33 (5-6): 533-40. PMID 12765698.
Geppetti P, Trevisani M (2004). "Activation and sensitisation of the vanilloid receptor: role in gastrointestinal inflammation and function.". Br. J. Pharmacol.141 (8): 1313-20. doi:10.1038/sj.bjp.0705768. PMID 15051629.
Clapham DE, Julius D, Montell C, Schultz G (2006). "International Union of Pharmacology. XLIX. Nomenclature and structure-function relationships of transient receptor potential channels.". Pharmacol. Rev.57 (4): 427-50. doi:10.1124/pr.57.4.6. PMID 16382100.
Szallasi A, Cruz F, Geppetti P (2007). "TRPV1: a therapeutic target for novel analgesic drugs?". Trends in molecular medicine12 (11): 545-54. doi:10.1016/j.molmed.2006.09.001. PMID 16996800.
Liddle RA (2007). "The role of Transient Receptor Potential Vanilloid 1 (TRPV1) channels in pancreatitis.". Biochim. Biophys. Acta1772 (8): 869-78. doi:10.1016/j.bbadis.2007.02.012. PMID 17428642.