Open AccessJournal Article
Cannabimimetic fatty acid derivatives: the anandamide family and other endocannabinoids.
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TLDR
The metabolic pathways suggested so far to underlie the biosynthesis and inactivation of anandamide and 2-AG and the current knowledge of the chemical bases for the interactions of an andamide with proteins of the endogenous cannabinoid system characterized so far are reviewed.Abstract:
In agreement with the highly lipophilic nature of (-)-Δ 9 -tetrahydrocannabinol, all the endogenous ligands of cannabinoid receptors identified so far are derivatives of long chain fatty acids. N- Arachidonoylethanolamine (anandamide) and some of its polyunsaturated congeners have been found in mammalian brain and shown to activate the CB1 and, with a lower efficacy, CB2 cannabinoid receptor subtypes. More recently, 2-arachidonoylglycerol (2-AG), a widespread intermediate in the metabolism of phosphoglycerides, diacylglycerols and triglycerides, was also found to activate the cannabinoid receptors. The capability of palmitoylethanolamide, an anti-inflammatory metabolite, to activate CB2-like receptors is still being debated. Here we review: 1) the metabolic pathways suggested so far to underlie the biosynthesis and inactivation of anandamide and 2-AG, and 2) the current knowledge of the chemical bases for the interactions of anandamide and 2-AG with proteins of the 'endogenous cannabinoid system' characterized so far, i.e. the CB1 and CB2 receptor subtypes, the membrane 'anandamide carrier', which facilitates anandamide diffusion into cells, and the enzyme 'fatty acid amide hydrolase', which catalyzes anandamide and, to a certain extent, 2-AG hydrolysis in vivo.read more
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Journal ArticleDOI
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
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Anti-Inflammatory, Antioxidant and Crystallographic Studies of N-Palmitoyl-ethanol Amine (PEA) Derivatives
Carmela Saturnino,Ada Popolo,Anna Ramunno,Simona Adesso,Michela Pecoraro,Maria Rosaria Plutino,Silvia Rizzato,Alberto Albinati,Stefania Marzocco,Marina Sala,Domenico Iacopetta,Maria Stefania Sinicropi +11 more
TL;DR: Biological evaluation of a small library of N-palmitoyl-ethanolamine analogues or derivatives, characterized by a protected acid function, useful to decrease their hydrolysis rate in vitro and prolong their biological activity are reported.
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Cannabinoid receptor signaling
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