Your browser version may not work well with NCBI's Web applications. More information here...
1: Eur J Pharmacol. 2000 May 12;396(1):39-42.
Related Articles, Links
Click here to read
The anandamide transport inhibitor AM404 activates vanilloid receptors.

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

Department of Clinical Pharmacology, Institute of Laboratory Medicine, Lund University, SE-221 85, Lund, Sweden. peter.zygmunt@klinfarm.lu.se

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.

Publication Types:
PMID: 10822052 [PubMed - indexed for MEDLINE]