4-O and 5-aminomethylation of synthetic capsaicin derivatives, a

Details 4-O and 5-aminomethylation of synthetic capsaicin derivatives, a 4-O and 5-aminomethylation of synthetic capsaicin derivatives, a

1995-10-23

1998-11-24

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544 90, C07D27301

Patent

active

058407200

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 ##STR1## wherein R is a member selected from the group consisting of ##STR2## wherein R.sub.1 is a member selected from the group consisting of C.sub.1-12 alkyl, C.sub.1-12 alkenyl, C.sub.1-12 alkylene, and C.sub.1-12 alkenylene, and
wherein R.sub.2 is a member selected from the group consisting of H, C.sub.1-3 alkylene-NR.sub.1 R.sub.1, and C.sub.1-6 alkenylene-NR.sub.1 R.sub.1.

REFERENCES:
patent: 3082112 (1963-03-01), Hemwall
patent: 4035363 (1977-07-01), Oka et al.
Ruthenium red antagonism of the effect of capsaicin on the motility of the isolated guinea-pig ileum, Takaki, Jin, and Nakayama, European Journal of Pharmacology, 174 (1989).
Capsazepine inhibits low pH- and lactic acid-evoked release of calcitonin gene-related peptide from sensory nerves in guinea-pig heart, Cereceda and Lundberg, European Journal of Pharmacology, 221 (1992).
Ruthenium-red inhibits CGRP release by capsaicin and resiniferatoxin but not by ouabain, bradykinin or nicotine in guinea-pig heart: correlation with effects on cardiac contractility, Cereceda, Lou, and Lundberg, Br. J. Pharmacol. (1991).
A comparison of capsazepine and ruthenium red as capsaicin antagonists in the rat isolated urinary bladder and vas deferens, Maggi, Bevan, Walpole, Rang, and Giuliani, Br. J. Pharmacol. (1993).

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