title: Specific inhibition of benzodiazepine receptor binding by some 1,2,3-triazole derivatives.
abstract: Certain 1,2,3-triazole derivatives were prepared and tested for their ability to displace [3H]diazepam from bovine brain membranes. From these compounds, the quinolytriazole derivatives (14, 15, 16, 17) were clearly the most potent, while the naphthyl- and the naphthyridyl-triazoles were considerably less active. The p-nitrophenyl derivative (15) was the compound that bound with the highest affinity within the quinolyltriazole compounds class. The replacement of the p-nitrophenyl group with other substituents greatly decreased the binding activity. From a Lineweaver-Burk analysis of 11, it appears that the inhibition is competitive.
authors.affiliation: Istituto Policattedra di Discipline Biologiche, Università di Pisa, Italy.
authors.forename: C
authors.initials: C
authors.lastname: Martini
authors.forename: W
authors.initials: W
authors.lastname: Marrucci
authors.forename: A
authors.initials: A
authors.lastname: Lucacchini
authors.forename: G
authors.initials: G
authors.lastname: Biagi
authors.forename: O
authors.initials: O
authors.lastname: Livi
mesh_terms: D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002417:Cattle; D055598:Chemical Phenomena; D002621:Chemistry; D003975:Diazepam / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D011963:Receptors, GABA-A / Q000187:drug effects*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000494:pharmacology*
chemical_list: D011963:Receptors, GABA-A; D014230:Triazoles; D003975:Diazepam