TRPV1 blocker / Vanilloid receptor I (TRPV1) antagonist, IC50 = 35 nM for capsaicin-induced and 6 nM for acid-induced TRPV1 activation. Displays analgesic activity in rat models of neuropathic pain. Orally active and cell permeable.
Biochemicals & reagents
393514-24-4
1) Valenzano et al. (2003), N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties; J. Pharmacol. Exp. Ther., 306 377 / 2) Pomonis et al. (2003), N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. in vivo characterization in rat models of inflammatory and neuropathic pain; J. Pharmacol. Exp. Ther., 306 387
RT
TARGET: Ion channel -- PATHWAY: Cation channel -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain