精神药物研究。IV. 1,3,4,14β-四氢-10-甲基-2H,10H-吡嗪并[2,1-d]吡咯并[1,2-b][1,2,5]苯并三氮杂䓬及其衍生物的合成与神经精神药理学效应
Researches on psychotropic agents. IV. Synthesis and neuropsychopharmacological effects of 1,3,4,14 b-tetrahydro-10-methyl-2H,10H- pyrazino[2,1-d] pyrrolo[1,2-b][1,2,5]benzotriazepine and its derivatives.
作者信息
Stefancich G, Artico M, Silvestri R, Pantaleoni G C, Giorgi R, Palumbo G
机构信息
Dipartimento di Scienze, Farmaceutiche, Università di Trieste, Italy.
出版信息
Farmaco. 1992 Jul-Aug;47(7-8):987-99.
The synthesis and neuropsychopharmacological properties of new 1,3,4,14b-tetrahydro-2H,10H-pyrazino [2,1-d] pyrrolo [1,2-b] [1,2,5] benzotriazepine derivatives related to antidepressant agent aptazepine are reported. The new derivatives displayed sedative-miorelaxant activity in mice, but no significant antagonist effect on clonidine blockade of phenylquinone-induced abdominal constriction. Among test compounds 4a, 4l and 4n showed high antinociceptive effect on the hot-plate test and compound 4e protected from death and convulsion all the electroshocked animals.
报道了与抗抑郁药阿普他泽平相关的新型1,3,4,14b-四氢-2H,10H-吡嗪并[2,1-d]吡咯并[1,2-b][1,2,5]苯并三氮杂卓衍生物的合成及其神经精神药理学特性。这些新型衍生物在小鼠中表现出镇静-肌松活性，但对可乐定阻断苯醌诱导的腹部收缩没有显著的拮抗作用。在测试化合物中，4a、4l和4n在热板试验中显示出高抗伤害感受作用，化合物4e可保护所有电休克动物免于死亡和惊厥。
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