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Volume 350, Issue 2-3 p. 240-244
Full-length article
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SR141716A, a potent and selective antagonist of the brain cannabinoid receptor

Murielle Rinaldi-Carmona

Murielle Rinaldi-Carmona

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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Francis Barth

Francis Barth

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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Michel Héaulme

Michel Héaulme

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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David Shire

David Shire

Sanofi Recherches, 31676 Labège, France

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Bernard Calandra

Bernard Calandra

Sanofi Recherches, 31676 Labège, France

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Christian Congy

Christian Congy

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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Serge Martinez

Serge Martinez

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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Jeanne Maruani

Jeanne Maruani

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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Gervais Néliat

Gervais Néliat

Cerep, Le Bois l'Evêque, 86600 Celle l'Evescault, France

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Daniel Caput

Daniel Caput

Sanofi Recherches, 31676 Labège, France

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Pascual Ferrara

Pascual Ferrara

Sanofi Recherches, 31676 Labège, France

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Philippe Soubrié

Philippe Soubrié

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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Jean Claude Brelière

Jean Claude Brelière

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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Gérard Le Fur

Gérard Le Fur

Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France

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First published: August 22, 1994
Citations: 1,384
Corresponding author. Fax: (33) 67 10 67 67.

Abstract

SR141716A is the first selective and orally active antagonist of the brain cannabinoid receptor. This compound displays nanomolar affinity for the central cannabinoid receptor but is not active on the peripheral cannabinoid receptor. In vitro, SR141716A antagonises the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes. After intraperitoneal or oral administration SR141716A antagonises classical pharmacological and behavioural effects of cannabinoid receptor agonists. This compound should prove to be a powerful tool for investigating the in vivo functions of the anandamide/cannabinoid system.