Acyclic Vanilloid Receptor Antagonist Based on Capsazepine

Capsaicin. the pungent component of chili pepper. opens a novel cation selective ion channel in the plasma membrane of peripheral sensory neurons. Capsaicin channel agonists induce pain upon topical application in the early stage. which is followed by a period of desensitization. Although the agonists have been studied as a analgesics, their initial irritancy became sever side effect. So competive antagonists have been pursued as a novel pharmacological agent for analgesics, rather than agonists. (omitted)