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The anandamide transport inhibitor AM404 activates vanilloid receptors

Zygmunt, Peter M. LU ; 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
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
  • 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
2019-09-04 04:44:55
@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},
  keyword      = {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},
  volume       = {396},
  year         = {2000},
}