Literature DB >> 10822052

The anandamide transport inhibitor AM404 activates vanilloid receptors.

P M Zygmunt1, H Chuang, P Movahed, D Julius, E D Högestätt.   

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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Year:  2000        PMID： 10822052     DOI： 10.1016/s0014-2999(00)00207-7

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  71 in total

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