TRPV1 is a member of a distinct subgroup of transient receptor potential (TRP) family of ion channels, highly expressed in primary nociceptors. TRPV1 can be activated by several different stimuli such as heat, acid, certain arachidonic acid derivatives and direct phosphorylation via PKC. TRPV1 may serve a central role in inflammatory nociception.
产品描述
An Antagonist of TRPV1 Channel
产品形式
BCTC (N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carbox-amide) is a potent, selective antagonist of the vanilloid receptor 1 (TRPV1) that is orally bioavailable. BCTC has the ability to block the activation of TRPV1 by capsaicin and also by low pH. It has an IC50 of 35 nM3. Oral administration of BCTC in rats significantly reduces mechanical and thermal hyperalgesia associated with inflammation or nerve injury.