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Anandamide, a Brain Endogenous Compound, Interacts Specifically with Cannabinoid Receptors and Inhibits Adenylate Cyclase
Author(s) -
Vogel Zvi,
Barg Jacob,
Levy Rivka,
Saya Danielle,
Heldman Eliahu,
Mechoulam Raphael
Publication year - 1993
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1993.tb03576.x
Subject(s) - anandamide , adenylate kinase , cyclase , cannabinoid , cannabinoid receptor , endocannabinoid system , endogeny , chemistry , receptor , neuroscience , pharmacology , microbiology and biotechnology , biochemistry , biology , antagonist
A putative endogenous cannabinoid ligand, arachidonylethanolamide (termed “anandamide”), was isolated recently from porcine brain. Here we demonstrate that this compound is a specific cannabinoid agonist and exerts its action directly via the cannabinoid receptors. Anandamide specifically binds to membranes from cells transiently (COS) or stably (Chinese hamster ovary) transfected with an expression plasmid carrying the cannabinoid receptor DNA but not to membranes from control non‐transfected cells. Moreover, anandamide inhibited the forskolin‐stimulated adenylate cyclase in the transfected cells and in cells that naturally express cannabinoid receptors (N 18 TG 2 neuroblastoma) but not in control nontransfected cells. As with exogenous cannabinoids, the inhibition by anandamide of the forskolin‐stimulated adenylate cyclase was blocked by treatment with pertussis toxin. These data indicate that anandamide is an endogenous agonist that may serve as a genuine neurotransmitter for the cannabinoid receptor.