The anandamide transport inhibitor AM404 activates vanilloid receptors |
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Authors: | Zygmunt P M Chuang H Movahed P Julius D Högestätt E D |
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Institution: | Department of Clinical Pharmacology, Institute of Laboratory Medicine, Lund University, SE-221 85, Lund, Sweden. peter.zygmunt@klinfarm.lu.se |
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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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