Tarzia G, Occelli E, Corsico N, Gallico L, Luzzani F, Barone D
Farmaco. 1989 Jan;44(1):17-28.
Some 2-aminoalkyl-8-chloro- and 2-aryl-1,2,4-triazolo[3,4-a]-phthalazine-3-(2H)-ones were synthesized and preliminarily tested in vitro and in vivo as potential benzodiazepine-receptor (BZRs) ligands. 2-Aryl-1,2,4-triazolo[3,4-a]-phthalazine-3(2H)-ones displaced in vitro 3H-diazepam (3H-DZ) from rat brain specific binding sites with Ki (nM) comparable to DZ and chlordiazepoxide used as reference compounds. The specific binding of the triazolones of this study was not enhanced in vitro by 4-aminobutyric acid (GABA) and in vivo they did not show any activity in counteracting the pentylenetetrazole (PTZ) induced convulsions (mice). One of these compounds (IV a) antagonized the effects of DZ in the bicuculline (BIC) induced convulsions test (mice) and the DZ induced muscle relaxant effects in the horizontal wire test.
合成了一些2-氨基烷基-8-氯-和2-芳基-1,2,4-三唑并[3,4-a] -酞嗪-3-(2H)-酮，并作为潜在的苯二氮䓬受体（BZR）配体进行了体外和体内初步测试。2-芳基-1,2,4-三唑并[3,4-a] -酞嗪-3(2H)-酮在体外从大鼠脑特异性结合位点置换3H-地西泮（3H-DZ），其Ki（nM）与用作参考化合物的地西泮和氯氮䓬相当。本研究中三唑酮的特异性结合在体外未被4-氨基丁酸（GABA）增强，并且在体内它们在对抗戊四氮（PTZ）诱导的惊厥（小鼠）中未显示任何活性。这些化合物之一（IV a）在荷包牡丹碱（BIC）诱导的惊厥试验（小鼠）中拮抗了地西泮的作用，并在水平钢丝试验中拮抗了地西泮诱导的肌肉松弛作用。
