title: Benzodiazepine receptor ligands. Synthesis and in vitro binding activity of some 6-substituted-3-aryl-1,2,4-triazolo[3,4-a]phthalazines.
abstract: Some 3-aryl-6-hydroxymethyl-1,2,4-triazolo[3,4-a]phthalazines (VI a,b) and 3-aryl-6-(2-hydroxyethyl)-1,2,4-triazolo[3,4-a]phthalazines (XVIII) have been synthesized. From (VI b) some 3-aryl-6-(alkylamino)methyl- and 3-aryl-6-(alkoxy)methyl-1,2,4-triazolo[3,4-a]phthalazines have been prepared and evaluated in vitro for their ability to inhibit selective 3H-diazepam (3H-DZ) binding to benzodiazepine-receptors (BZRs) from homogenates of synaptosomes from rat brains. Several compounds have been shown to displace 3H-DZ from BZRs with Ki (nM) values ranging from 2.2 to 88, comparable to those of the reference drugs including Diazepam.
authors.forename: G
authors.initials: G
authors.lastname: Tarzia
authors.forename: E
authors.initials: E
authors.lastname: Occelli
authors.forename: D
authors.initials: D
authors.lastname: Barone
mesh_terms: D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D010793:Phthalazines / Q000138:chemical synthesis*; D011724:Pyridazines / Q000138:chemical synthesis*; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000378:metabolism*; D014230:Triazoles / Q000138:chemical synthesis*
chemical_list: D010793:Phthalazines; D011724:Pyridazines; D011963:Receptors, GABA-A; D014230:Triazoles