Title : 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.

Pub. Date : 2003 Jul

PMID : 12721338






4 Functional Relationships(s)
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1 Vanilloids such as capsaicin have algesic properties and seem to mediate their effects via activation of the vanilloid receptor 1 (VR1), a ligand-gated ion channel highly expressed on primary nociceptors. Capsaicin transient receptor potential cation channel, subfamily V, member 1 Rattus norvegicus
2 Vanilloids such as capsaicin have algesic properties and seem to mediate their effects via activation of the vanilloid receptor 1 (VR1), a ligand-gated ion channel highly expressed on primary nociceptors. Capsaicin transient receptor potential cation channel, subfamily V, member 1 Rattus norvegicus
3 Although blockade of capsaicin-induced VR1 activation has been demonstrated in vitro and in vivo with the antagonist capsazepine, efficacy in rat models of chronic pain has not been observed with this compound. Capsaicin transient receptor potential cation channel, subfamily V, member 1 Rattus norvegicus
4 Similar to capsazepine, this compound inhibits capsaicin-induced activation of rat VR1 with an IC50 value of 35 nM. Capsaicin transient receptor potential cation channel, subfamily V, member 1 Rattus norvegicus