Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5976
DC FieldValueLanguage
dc.contributor.authorBrizzi, Antonellaen_us
dc.contributor.authorCASCIO M., Gen_us
dc.contributor.authorFrosini, Mariaen_us
dc.contributor.authorLigresti, Aen_us
dc.contributor.authorAiello, Fen_us
dc.contributor.authorBiotti, Ien_us
dc.contributor.authorBrizzi, Vittorioen_us
dc.contributor.authorPERTWEE R., Gen_us
dc.contributor.authorCorelli, Federicoen_us
dc.contributor.authorDI MARZO, V.en_us
dc.date.accessioned2021-03-30T15:56:32Z-
dc.date.available2021-03-30T15:56:32Z-
dc.date.issued2011-
dc.identifier.issn0022-2623en_US
dc.identifier.urihttp://hdl.handle.net/20.500.12779/5976-
dc.description21890en_US
dc.description.abstractSince 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.en_US
dc.language.isoenen_US
dc.relationNoneen_US
dc.relation.ispartofJOURNAL OF MEDICINAL CHEMISTRYen_US
dc.titleResorcinol-sn-Glycerol Derivatives: Novel 2-Arachidonoylglycerol (2-AG) Mimetics Endowed with High Affinity and Selectivity for Cannabinoid Type 1 (CB1) Receptoren_US
dc.typeArticleen_US
dc.identifier.doi10.1021/jm200529hen_US
dc.identifier.pmid22044209en_US
dc.identifier.scopus2-s2.0-84055221870en_US
dc.identifier.isiWOS:000297946300005en_US
dc.relation.volume54en_US
dc.relation.issue24en_US
dc.description.firstpage8278en_US
dc.description.lastpage8288en_US
dc.description.thirdmissionNot applicableen_US
item.cerifentitytypePublications-
item.grantfulltextnone-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeArticle-
item.fulltextNo Fulltext-
crisitem.author.orcid0000-0002-2310-9899-
crisitem.author.orcid0000-0002-5750-4504-
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