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TRPV1<br />
• The transient receptor potential cation<br />
channel, subfamily V, member 1 also known<br />
as TRPV1 is a ligand-gated nonselective<br />
cation channel that may be activated by a<br />
wide variety of exogenous and endogenous<br />
physical and chemical stimuli, including heat<br />
greater than 43°C, low pH (acidic<br />
conditions), <strong>the</strong> endocannabinoid<br />
anandamide, N-arachidonoyl-dopamine, and<br />
capsaicin.<br />
• TRPV1 receptors are found in <strong>the</strong> central<br />
nervous system and <strong>the</strong> peripheral nervous<br />
system and are involved in <strong>the</strong> transmission<br />
and modulation of pain, as well as <strong>the</strong><br />
integration of diverse painful stimuli.<br />
• TRPV1 blockade in vivo elicits hyper<strong>the</strong>rmia<br />
in multiple species, from rodents to humans,<br />
suggesting that TRPV1 is involved in body<br />
temperature maintenance.<br />
73<br />
Nature Reviews Drug Discovery Vol.6 May 2007<br />
© Defined Health, 2009<br />
Pain Insight Briefing<br />
Homology model of <strong>the</strong> TRPV1 ion channel<br />
tetramer (w<strong>here</strong> <strong>the</strong> monomers are individually<br />
colored cyan, green, blue, and magenta<br />
respective) imbedded in a cartoon re<strong>presentation</strong><br />
of a lipid bilayer. PIP2 signaling ligands are<br />
represented by space-filling models (carbon =<br />
white, oxygen = red, phosphorous = orange).
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