The anandamide transport inhibitor AM404 activates vanilloid receptors
(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
- Zygmunt, Peter M. LU ; Chuang, Huai Hu ; Movahed, Pouya ; Julius, David and Högestätt, Edward D. LU
- organization
- publishing date
- 2000-05-12
- 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
- 2024-10-02 03:08:35
@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}}, }