title: Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif.
abstract: A new series of 1,2,4-triazoles have been prepared and the evaluation of their cannabinoid properties have been carried out. Compound 8 showed cannabinoid silent antagonist activity in mouse vas deferens and guinea pig ileum preparations and in vivo assays (cannabinoid tetrad) in mouse. It did not have intrinsic activity in these bioassays, and therefore, it did not behave as a partial agonist or an inverse agonist.
authors.affiliation: Instituto de Química Médica, Consejo Superior de Investigaciones Científicas, Juan de la Cierva, 3, E-28006 Madrid, Spain. nadine@iqm.csic.es
authors.forename: Nadine
authors.initials: N
authors.lastname: Jagerovic
authors.forename: Laura
authors.initials: L
authors.lastname: Hernandez-Folgado
authors.forename: Ibon
authors.initials: I
authors.lastname: Alkorta
authors.forename: Pilar
authors.initials: P
authors.lastname: Goya
authors.forename: Miguel
authors.initials: M
authors.lastname: Navarro
authors.forename: Antonia
authors.initials: A
authors.lastname: Serrano
authors.forename: Fernando
authors.initials: F
authors.lastname: Rodriguez de Fonseca
authors.forename: M Teresa
authors.initials: MT
authors.lastname: Dannert
authors.forename: Angela
authors.initials: A
authors.lastname: Alsasua
authors.forename: Margarita
authors.initials: M
authors.lastname: Suardiaz
authors.forename: David
authors.initials: D
authors.lastname: Pascual
authors.forename: Maria Isabel
authors.initials: MI
authors.lastname: Martín
mesh_terms: D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001667:Binding, Competitive; D063386:Cannabinoid Receptor Agonists; D063387:Cannabinoid Receptor Antagonists; D002531:Cerebellum / Q000378:metabolism; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D011869:Radioligand Assay; D051381:Rats; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014649:Vas Deferens / Q000187:drug effects / Q000502:physiology
chemical_list: D063386:Cannabinoid Receptor Agonists; D063387:Cannabinoid Receptor Antagonists; D014230:Triazoles