Journal ArticleDOI
The anandamide transport inhibitor AM404 activates vanilloid receptors.
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TLDR
In conclusion, AM404 activates native and cloned vanilloid receptors and causes vasodilation in rat isolated hepatic artery contracted with phenylephrine.About:
This article is published in European Journal of Pharmacology.The article was published on 2000-05-12. It has received 253 citations till now. The article focuses on the topics: TRPV1 & Cannabinoid.read more
Citations
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International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors
Allyn C. Howlett,Francis Barth,Tom I. Bonner,Guy A. Cabral,Pierre Casellas,William A. Devane,Christian C. Felder,Miles Herkenham,Ken Mackie,Billy R. Martin,Raphael Mechoulam,Roger G. Pertwee +11 more
TL;DR: It is considered premature to rename cannabinoid receptors after an endogenous agonist as is recommended by the International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification, because pharmacological evidence for the existence of additional types of cannabinoid receptor is emerging and other kinds of supporting evidence are still lacking.
Journal ArticleDOI
The Endocannabinoid System as an Emerging Target of Pharmacotherapy
TL;DR: A comprehensive overview on the current state of knowledge of the endocannabinoid system as a target of pharmacotherapy is provided.
Journal ArticleDOI
The Vanilloid Receptor: A Molecular Gateway to the Pain Pathway
Michael J. Caterina,David Julius +1 more
TL;DR: The analysis of vanilloid receptor gene knockout mice confirms the involvement of this channel in pain sensation, as well as in hypersensitivity to noxious stimuli following tissue injury, and demonstrates the existence of redundant mechanisms for the sensation of heat-evoked pain.
Journal ArticleDOI
Targeting the endocannabinoid system: to enhance or reduce?
TL;DR: The discovery of compounds that either prolong the lifespan of endocannabinoids or tone down their action for the potential future treatment of pain, affective and neurodegenerative disorders, gastrointestinal inflammation, obesity and metabolic dysfunctions, cardiovascular conditions and liver diseases is discovered.
Journal ArticleDOI
Drugs, their targets and the nature and number of drug targets
TL;DR: This work considers the nature of drug targets, and by classifying known drug substances on the basis of the discussed principles it provides an estimation of the total number of current drug targets.
References
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Journal ArticleDOI
The capsaicin receptor: a heat-activated ion channel in the pain pathway
Michael J. Caterina,Mark Schumacher,Makoto Tominaga,Tobias A. Rosen,Jon D. Levine,David Julius +5 more
TL;DR: The cloned capsaicin receptor is also activated by increases in temperature in the noxious range, suggesting that it functions as a transducer of painful thermal stimuli in vivo.
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Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide
Peter M. Zygmunt,Jesper Petersson,David Andersson,Huai-hu Chuang,Morten Sørgård,Vincenzo Di Marzo,David Julius,Edward D. Högestätt +7 more
TL;DR: It is shown that the vasodilator response to anandamide in isolated arteries is capsaicin-sensitive and accompanied by release of calcitonin-gene-related peptide (CGRP), which indicates that the vanilloid receptor may be another molecular target for endogenousAnandamide, besides cannabinoid receptors, in the nervous and cardiovascular systems.
Journal ArticleDOI
Pharmacology of cannabinoid cb1 and cb2 receptors
TL;DR: This review focuses on the classification, binding properties, effector systems and distribution of cannabinoid receptors, and describes the various cannabinoid receptor agonists and antagonists now available and considers the main in vivo and in vitro bioassay methods that are generally used.
Journal ArticleDOI
Functional Role of High-Affinity Anandamide Transport, as Revealed by Selective Inhibition
Massimiliano Beltramo,N. Stella,N. Stella,N. Stella,A. Calignano,A. Calignano,A. Calignano,Sonyuan Lin,Sonyuan Lin,Sonyuan Lin,Alexandros Makriyannis,Alexandros Makriyannis,Alexandros Makriyannis,Daniele Piomelli,Daniele Piomelli,Daniele Piomelli +15 more
TL;DR: The data indicate that carrier-mediated transport may be essential for termination of the biological effects of anandamide, and may represent a potential drug target.
Journal ArticleDOI
Capsazepine: a competitive antagonist of the sensory neurone excitant capsaicin.
Stuart Bevan,S. Hothi,Glyn Hughes,Iain F. James,Humphrey P. Rang,Kirti Shah,Walpole Christopher,J.C. Yeats +7 more
TL;DR: The present study shows the capsazepine acts as a competitive antagonist of capsaicin, with significant effects on the efflux of 86Rb+ from cultured DRG neurones evoked either by depolarization with high (50 mm) K+ solutions or by acidification of the external medium to pH 5.6.