abstract |
A series of 4-O & 5-aminomethylation of synthetic capsaicin derivatives selectively reveal antagonist activity on capsaicin-sensitive sensory neurons, and inhibit its innervating atrium, airway, and ileum smooth muscles in vitro. The compound of this invention has the following formula <IMAGE> wherein R is a member selected from the group consisting of <IMAGE> <IMAGE> <IMAGE> <IMAGE> <IMAGE> <IMAGE> wherein R1 is a member selected from the group consisting of C1-12 alkyl, C1-12 alkenyl, C1-12 alkylene, and C1-12 alkenylene, and wherein R2 is a member selected from the group consisting of H, C1-3 alkylene-NR1R1, and C1-6 alkenylene-NR1R1. |