Reactome | TRPV1 binds TRPV1 blockers

TRPV1 binds TRPV1 blockers

Stable Identifier

R-HSA-9701147

Type

Reaction [binding]

Species

Homo sapiens

Compartment

extracellular region, plasma membrane

ReviewStatus

5/5

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Capsazepine is a synthetic antagonist of capsaicin. It is used as a biochemical tool in the study of TRPV ion channels (Valenzano & Sun 2004). Capsazepine blocks the painful sensation of heat caused by capsaicin which activates the TRPV1 ion channel (Bevan et al. 1992). Another potent TRPV1 channel blocker is ruthenium red, used as another tool for TRPV channel pharmacology (McIntyre et al. 2001, Smart et al. 2001). Antagonists of PRPV1 have yet to reach the clinic. While capsazepine has proven a useful tool for unraveling the molecular pharmacology of TRPV1, in vivo studies have had limited success due to poor pharmacokinetic properties and species selectivity (Valenzano & Sun 2004).

Literature References

PubMed ID	Title	Journal	Year
11301059	Characterisation using FLIPR of human vanilloid VR1 receptor pharmacology Ranson, J, Smart, D, Gunthorpe, MJ, Jerman, JC, Davis, JB, Randall, AD, Hayes, PD, Cairns, W, Brough, SJ	Eur. J. Pharmacol.	2001
11226139	Pharmacological differences between the human and rat vanilloid receptor 1 (VR1) Rang, HP, Winter, J, Toms, C, Chambers, A, McLatchie, LM, Weerasakera, N, McIntyre, P, Clarke, M, James, IF, Peacock, M, Savidge, J, Phillips, E, Webb, M, Shah, K, Bevan, S	Br. J. Pharmacol.	2001
1422598	Capsazepine: a competitive antagonist of the sensory neurone excitant capsaicin Rang, HP, James, IF, Hothi, S, Yeats, JC, Shah, K, Bevan, S, Walpole, CS, Hughes, G	Br. J. Pharmacol.	1992