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…

Index: 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

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Citation Number: 15

Abstract

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 ...