Specific inhibition of benzodiazepine receptor binding by some 6H-indolo[2,3-b] [1,8]naphthyridines and 11H-indolo [3,2-c] [1,8]naphthyridines.
The reactivity of some 6H-indolo[2,3-b] [1,8]naphthyridines (II) and 11H-indolo[3,2-c] [1,8]naphthyridines (III) in displacing specific [3H] diazepam binding from bovine brain membranes was examined. All the indolonaphthyridines tested are active and show a higher activity than indole and tryptophan. The inhibition is due to direct interaction with the benzodiazepine binding sites. Some structure-activity relationships are discussed.
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D002417:Cattle; D003975:Diazepam / Q000378:metabolism; D066298:In Vitro Techniques; D007211:Indoles / Q000378:metabolism; D007700:Kinetics; D009287:Naphthyridines / Q000378:metabolism*; D011956:Receptors, Cell Surface / Q000187:drug effects*; D011963:Receptors, GABA-A
D007211:Indoles; D009287:Naphthyridines; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D003975:Diazepam