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The anandamide transport inhibitor AM404 activates vanilloid receptors

Zygmunt, Peter M. LU orcid ; Chuang, Huai Hu ; Movahed, Pouya ; Julius, David and Högestätt, Edward D. LU (2000) In European Journal of Pharmacology 396(1). p.39-42
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... (More)

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. Copyright (C) 2000 Elsevier Science B.V.

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author
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organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Afferent, Cannabinoid, Capsaicin, Neuron, Pain, Receptor, Sensory, Vasodilation
in
European Journal of Pharmacology
volume
396
issue
1
pages
4 pages
publisher
Elsevier
external identifiers
  • pmid:10822052
  • scopus:0034640192
ISSN
0014-2999
DOI
10.1016/S0014-2999(00)00207-7
language
English
LU publication?
yes
id
dd40c882-13aa-4caa-9142-9cd9b0054f88
date added to LUP
2019-05-31 21:31:52
date last changed
2025-10-16 23:55:44
@article{dd40c882-13aa-4caa-9142-9cd9b0054f88,
  abstract     = {{<p>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. Copyright (C) 2000 Elsevier Science B.V.</p>}},
  author       = {{Zygmunt, Peter M. and Chuang, Huai Hu and Movahed, Pouya and Julius, David and Högestätt, Edward D.}},
  issn         = {{0014-2999}},
  keywords     = {{Afferent; Cannabinoid; Capsaicin; Neuron; Pain; Receptor; Sensory; Vasodilation}},
  language     = {{eng}},
  month        = {{05}},
  number       = {{1}},
  pages        = {{39--42}},
  publisher    = {{Elsevier}},
  series       = {{European Journal of Pharmacology}},
  title        = {{The anandamide transport inhibitor AM404 activates vanilloid receptors}},
  url          = {{http://dx.doi.org/10.1016/S0014-2999(00)00207-7}},
  doi          = {{10.1016/S0014-2999(00)00207-7}},
  volume       = {{396}},
  year         = {{2000}},
}