http://www.cnr.it/ontology/cnr/individuo/prodotto/ID196981

An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity (Articolo in rivista)

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An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity (Articolo in rivista) (literal)

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Alternative label

Ben-Shabat S, Fride E, Sheskin T, Tamiri T, Rhee MH, Vogel Z, Bisogno T, De Petrocellis L, Di Marzo V, Mechoulam R. (1998)
An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity
in European journal of pharmacology; ELSEVIER SCIENCE BV, PO BOX 211, 1000 AE AMSTERDAM, NETHERLANDS, AMSTERDAM (Paesi Bassi)
(literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

Ben-Shabat S, Fride E, Sheskin T, Tamiri T, Rhee MH, Vogel Z, Bisogno T, De Petrocellis L, Di Marzo V, Mechoulam R. (literal)

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1. Hebrew Univ Jerusalem, Fac Med, Dept Nat Prod, David Bloom Ctr Pharm, IL-91120 Jerusalem, Israel 2. Israel Police Headquarters, Div Identificat & Forens Sci, Jerusalem, Israel 3. Weizmann Inst Sci, Dept Neurobiol, IL-76100 Rehovot, Israel 4. CNR, Ist Chim Mol Interesse Biol, I-80072 Arco Felice Napoli, Naples, Italy 5. CNR, Ist Cibernetica, I-80072 Arco Felice Napoli, Naples, Italy (literal)

Titolo

An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity (literal)

Abstract

2-Arachidonoyl-glycerol (2-Ara-G1) has been isolated from various tissues and identified as an endogenous ligand for both cannabinoid receptors, CB1 and CB2. Here we report that in spleen, as in brain and gut, 2-Ara-G1 is accompanied by several 2-acyl-glycerol esters, two major ones being 2-linoleoyl-glycerol (2-Lino-G1) and 2-palmitoyl-glycerol (2-Palm-G1). These two esters do not bind to the cannabinoid receptors, nor do they inhibit adenylyl cyclase via either CB1 or CB2; however, they significantly potentiate the apparent binding of 2-Ara-G1 and its apparent capacity to inhibit adenylyl cyclase. Together these esters also significantly potentiate 2-Ara-G1 inhibition of motor behavior, immobility on a ring, analgesia on a hot plate and hypothermia caused by 2-Ara-G1 in mice. 2-Lino-G1, but not 2-Palm-G1, significantly inhibits the inactivation of 2-Ara-G1 by neuronal and basophilic cells. These data indicate that the biological activity of 2-Ara-G1 can be increased by related, endogenous 2-acyl-glycerols, which alone show no significant activity in any of the tests employed. This effect ('entourage effect') may represent a novel route for molecular regulation of endogenous cannabinoid activity. (literal)

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