Chemical Name:N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihy
droxy-2H-2-benzazepine-2-carbothioamide
Biological Activity:
Selective vanilloid receptor
antagonist (Ki = 3.2 μM).
Inhibits carrageenan inflammation-induced hyperalgesic responses in the rat.
Also activates amiloride-sensitive epithelial Na+ channel ENaCδ.
Dickenson and Dray (1991) Selective antagonism of capsaicin by
capsazepine: evidence for a spinal receptor site in capsaicin-induced
antinociception. Br.J.Pharmacol. 104 1045. Kwaket al
(1998) A capsaicin-receptor antagonist, capsazepine, reduces
inflammation-induced hyperalgesic responses in the rat: evidence for an
endogenous capsaicin-like substance. Neuroscience 86 619.
Yamamuraet al (2004) Capsazepine is a novel activator of the δ
subunit of the human epithelial Na+ channel. J.Biol.Chem. 279
44483.