Benzodiazepine receptor ligands. Synthesis and pharmacological evaluation of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines.
A series of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines was synthesised starting from suitable o-benzoylbenzoic acids. The compounds were tested in vitro for inhibition of the specific binding of 3H-Diazepam to benzodiazepine receptors in preparations of membranes from rat brain synaptosomes. None of the compounds was notably active in this test.
Tarzia
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Merrell Dow Research Institute, Lepetit Research Center, Gerenzano, Italy.
Occelli
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Barone
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D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism; D008297:Male; D051379:Mice; D010793:Phthalazines / Q000138:chemical synthesis* / Q000378:metabolism; D011724:Pyridazines / Q000138:chemical synthesis*; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013574:Synaptosomes / Q000378:metabolism; D014230:Triazoles / Q000138:chemical synthesis* / Q000378:metabolism
D010793:Phthalazines; D011724:Pyridazines; D011963:Receptors, GABA-A; D014230:Triazoles; D003975:Diazepam