A novel agonist, phorbol 12-phenylacetate 13-acetate 20-homovanillate, abolishes positive cooperativity of binding by the vanilloid receptor

…, G Acs, G Cravotto, PM Blumberg, JM Lundberg…

文献索引：Szallasi, Arpad; Acs, Geza; Cravotto, Giancarlo; Blumberg, Peter M.; Lundberg, Jan M.; Appendino, Giovanni European Journal of Pharmacology, 1996 , vol. 299, # 1-3 p. 221 - 228

全文：HTML全文

被引用次数: 15

摘要

Capsaicin binds to a specific recognition site, referred to as the vanilloid receptor, which it shares with the natural, ultrapotent agonist resiniferatoxin and with the competitive antagonist capsazepine. Upon binding to its receptor, capsaicin opens a cation channel leading to Ca2+ influx. The binding of capsaicin or resiniferatoxin by the vanilloid receptor follows a sigmoidal saturation curve, indicative of positive cooperativity. The biological ...