Article
Identification of species-specific determinants of the action of the antagonist capsazepine and the agonist PPAHV on TRPV1.
The Journal of biological chemistry - 23 Apr 2004
Phillips Elsa, Reeve Alison, Bevan Stuart, McIntyre Peter
Abstract excerpt
The vanilloid receptor 1 (VR1 or TRPV1) ion channel is activated by noxious heat, low pH and by a variety of vanilloid-related compounds. The antagonist, capsazepine is more effective at inhibiting the human TRPV1 response to pH 5.5 than the rat TRPV1 response to this stimulus. Mutation of rat TRPV1 at three positions in the S3 to S4 region, to the corresponding human amino acid residues I514M, V518L, and M547L...
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