6-(Alkylamino)-3-aryl-1, 2, 4-triazolo [3, 4-a] phthalazines. A new class of benzodiazepine receptor ligands

…, E Occelli, E Toja, D Barone, N Corsico…

Index: Tarzia, Giorgio; Occelli, Emilio; Toja, Emilio; Barone, Domenico; Corsico, Nerina; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 6 p. 1115 - 1123

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Citation Number: 55

Abstract

Some 6-(alkylamino)-3-aryl-1, 2, 4-triazolo [3, 4-a] phthalazines have been shown to displace diazepam from rat brain specific binding sites, in vitro, with Ki (nM) values comparable to those of reference benzodiazepines and to have anticonvulsant (pentylenetetrazole test, mice) and anticonflict activity (Vogel test, rat) in vivo. Separation between the doses causing anticonflict effects (Vogel test, rat) and those impairing motor ...