Specific inhibition of benzodiazepine receptor binding by some 1,2,3-triazole derivatives.
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.
Martini
C
C
Istituto Policattedra di Discipline Biologiche, Università di Pisa, Italy.
Marrucci
W
W
Lucacchini
A
A
Biagi
G
G
Livi
O
O
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*
D011963:Receptors, GABA-A; D014230:Triazoles; D003975:Diazepam