Synthesis and evaluation of phorboid 20-homovanillates: discovery of a class of ligands binding to the vanilloid (capsaicin) receptor with different degrees of …

…, G Cravotto, G Palmisano, R Annunziata…

文献索引：Appendino, Giovanni; Cravotto, Giancarlo; Palmisano, Giovanni; Annunziata, Rita; Szallasi, Arpad Journal of Medicinal Chemistry, 1996 , vol. 39, # 16 p. 3123 - 3131

全文：HTML全文

被引用次数: 40

摘要

A number of phorboid 20-homovanillates were prepared by condensation of phorbol 12, 13- diesters and 12-dehydrophorbol 13-esters with Mem-homovanillic acid followed by removal of the protecting group with SnCl4 in THF. These compounds were evaluated for their ability to inhibit [3H] resiniferatoxin (RTX) binding to rat spinal cord membranes. Compounds bearing a lipophilic ester group on ring C were considerably active, but a surprising ...