Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation (Articolo in rivista)

Type
Label
  • Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation (Articolo in rivista) (literal)
Anno
  • 2008-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.ejmech.2007.02.023 (literal)
Alternative label
  • Ortar Giorgio; Cascio Maria Grazia; Moriello Aniello Schiano; Camalli Mercedes; Morera Enrico; Nalli Marianna; Di Marzo Vincenzo (2008)
    Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation
    in European journal of medicinal chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Ortar Giorgio; Cascio Maria Grazia; Moriello Aniello Schiano; Camalli Mercedes; Morera Enrico; Nalli Marianna; Di Marzo Vincenzo (literal)
Pagina inizio
  • 62 (literal)
Pagina fine
  • 72 (literal)
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  • 43 (literal)
Rivista
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  • 1 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • CNR IC (literal)
Titolo
  • Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation (literal)
Abstract
  • We have synthesized a series of 18 1,5- and 2,5-disubstituted carbamoyl tetrazoles, including LY2183240 (1) and LY2318912 (7), two compounds previously described as potent inhibitors of the cellular uptake of the endocannabinoid anandamide, and their regioisomers 2 and 8. We confirm that compound 1 is a potent inhibitor of both the cellular uptake and, like the other new compounds synthesized here, the enzymatic hydrolysis of anandamide. With the exception of 9, 12, 15, and the 2,5-regioisomer of LY2183240 2, the other compounds,were all found to be weakly active or inactive on anandamide uptake. Several compounds also inhibited the enzymatic hydrolysis of the other main endocannabinoid, 2-arachidonoylglycerol, as well as its enzymatic release from sn-1-oleoyl-2-arachidonoyl-glycerol, at submicromolar concentrations. Four of the novel compounds, i.e. 3, 4, 17, and 18, inhibited anandamide hydrolysis potently (IC(50) = 2.1-5.4 nM) and selectively over all the other targets tested (IC(50) >= 10 mu M), thus representing new potentially useful tools for the inhibition of fatty acid amide hydrolase. (C) 2007 Elsevier Masson SAS. All rights reserved. (literal)
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