The Anandamide Transport Inhibitor AM404 Activates Vanilloid Receptors

Overview

Journal Eur J Pharmacol

Specialty Pharmacology

Date 2000 May 24

PMID 10822052

Citations 83

Authors

P M Zygmunt

H Chuang

P Movahed

D Julius

E D Hogestatt

Affiliations

Soon will be listed here.

Abstract

The possibility that the anandamide transport inhibitor N-(4-hydroxyphenyl)-5,8,11,14-eicosatetraenamide (AM404), structurally similar to the vanilloid receptor agonists anandamide and capsaicin, may also activate vanilloid receptors and cause vasodilation was examined. AM404 evoked concentration-dependent relaxations in segments of rat isolated hepatic artery contracted with phenylephrine. Relaxations were abolished in preparations pre-treated with capsaicin. The calcitonin-gene related peptide (CGRP) receptor antagonist CGRP-(8-37) also abolished relaxations. The vanilloid receptor antagonist capsazepine inhibited vasodilation by AM404 and blocked AM404-induced currents in patch-clamp experiments on Xenopus oocytes expressing the vanilloid subtype 1 receptor (VR1). In conclusion, AM404 activates native and cloned vanilloid receptors.

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