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XB-ART-10972
Eur J Pharmacol 2000 May 12;3961:39-42. doi: 10.1016/s0014-2999(00)00207-7.
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The anandamide transport inhibitor AM404 activates vanilloid receptors.

Zygmunt PM , Chuang H , Movahed P , Julius D , Högestätt ED .


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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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Species referenced: Xenopus
Genes referenced: calca