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Originally published In Press as doi:10.1074/jbc.M008555200 on January 26, 2001

J. Biol. Chem., Vol. 276, Issue 16, 12856-12863, April 20, 2001
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The Activity of Anandamide at Vanilloid VR1 Receptors Requires Facilitated Transport across the Cell Membrane and Is Limited by Intracellular Metabolism*

Luciano De PetrocellisDagger §, Tiziana Bisogno§, Mauro Maccarrone||, John B. Davis**, Alessandro Finazzi-Agrò||, and Vincenzo Di MarzoDagger Dagger

From the  Endocannabinoid Research Group, Istituto per la Chimica di Molecole di Interesse Biologico and the Dagger  Istituto di Cibernetica, C. N. R., Via Toiano 6, 80072, Arco Felice, Napoli, Italy, the || Department of Experimental Medicine and Biochemical Sciences, University of Rome Tor Vergata, Italy, and ** Neurology, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom

The endogenous ligand of CB1 cannabinoid receptors, anandamide, is also a full agonist at vanilloid VR1 receptors for capsaicin and resiniferatoxin, thereby causing an increase in cytosolic Ca2+ concentration in human VR1-overexpressing (hVR1-HEK) cells. Two selective inhibitors of anandamide facilitated transport into cells, VDM11 and VDM13, and two inhibitors of anandamide enzymatic hydrolysis, phenylmethylsulfonyl fluoride and methylarachidonoyl fluorophosphonate, inhibited and enhanced, respectively, the VR1-mediated effect of anandamide, but not of resiniferatoxin or capsaicin. The nitric oxide donor, sodium nitroprusside, known to stimulate anandamide transport, enhanced anandamide effect on the cytosolic Ca2+ concentration. Accordingly, hVR1-HEK cells contain an anandamide membrane transporter inhibited by VDM11 and VDM13 and activated by sodium nitroprusside, and an anandamide hydrolase activity sensitive to phenylmethylsulfonyl fluoride and methylarachidonoyl fluorophosphonate, and a fatty acid amide hydrolase transcript. These findings suggest the following. (i) Anandamide activates VR1 receptors by acting at an intracellular site. (ii) Degradation by fatty acid amide hydrolase limits anandamide activity on VR1; and (iii) the anandamide membrane transporter inhibitors can be used to distinguish between CB1 or VR1 receptor-mediated actions of anandamide. By contrast, the CB1 receptor antagonist SR141716A inhibited also the VR1-mediated effect of anandamide and capsaicin on cytosolic Ca2+ concentration, although at concentrations higher than those required for CB1 antagonism.

* This work was supported in part by Ministero dell Università e della Ricerca Scientifica e Tecnologica Grant 3933 (to V. D. M.).The costs of publication of this article were defrayed in part by the payment of page charges. The article must therefore be hereby marked "advertisement" in accordance with 18 U.S.C. Section 1734 solely to indicate this fact.

§ These authors contributed equally to this work.

Dagger Dagger To whom correspondence should be addressed. Tel.: 39-081-853-4156; Fax: 39-081-804-1770; E-mail: vdimarzo@icmib.na.cnr.it.

Copyright © 2001 by The American Society for Biochemistry and Molecular Biology, Inc.
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