Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5976
Title: Resorcinol-sn-Glycerol Derivatives: Novel 2-Arachidonoylglycerol (2-AG) Mimetics Endowed with High Affinity and Selectivity for Cannabinoid Type 1 (CB1) Receptor
Authors: Brizzi, Antonella 
CASCIO M., G
Frosini, Maria
Ligresti, A
Aiello, F
Biotti, I
Brizzi, Vittorio
PERTWEE R., G
Corelli, Federico 
DI MARZO, V.
Issue Date: 2011
Project: None 
Journal: JOURNAL OF MEDICINAL CHEMISTRY
Abstract: 
Since the discovery of the endocannabinoid system, evidence has been progressively accumulating to suggest that 2-arachidonoylglycerol (2-AG) rather than anandamide (AEA) is the endogenous ligand for both cannabinoid (CB) receptors. Moreover, other studies have shown that another lipid molecule, 2-arachidonyl-glycerol ether (2-AGE, noladin ether), which acts as a full agonist at cannabinoid receptors, might occur in tissues. Having previously designed a resorcinol AEA hybrid model, in this paper we have explored the cannabinoid receptor binding properties, the CB, functional activity, and the stability to plasma esterases of a novel series of compounds characterized by the conversion of the amide head into the glycerol-ester or glycerol-ether head, typical of 2-AG or the "putative" endocannabinoid 2-AGE, respectively. Glyceryl esters 39 and 41 displayed greater potency for CB, (K, in the nanomolar range) than for CB2 receptors plus the potential to be exploited as useful hits for the development of novel 2-AG mimetics.
Description: 
21890
URI: http://hdl.handle.net/20.500.12779/5976
ISSN: 0022-2623
DOI: 10.1021/jm200529h
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