BENZODIAZEPINE ANTAGONIST RO 15-1788 - NEUROLOGICAL AND BEHAVIORAL-EFFECTS
BENZODIAZEPINE ANTAGONIST RO 15-1788 - NEUROLOGICAL AND BEHAVIORAL-EFFECTS
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DOI：
10.1007/bf00470579
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发表时间：
1982-01-01
影响因子：
3.4
通讯作者：
HAEFELY, W
中科院分区：
文献类型：
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作者：
BONETTI, EP;PIERI, L;HAEFELY, W
在小鼠、大鼠、狗和松鼠猴的神经学和行为学研究中，咪唑苯二氮卓酮ro15 -1788是一种有效的苯二氮卓类拮抗剂。拮抗活性是预防性和治疗性的，并且在没有检测到内在效应的剂量下观察到。它具有高度选择性，因为它对苯二氮卓类药物引起的中枢神经系统影响起作用，但对其他抑制剂如苯巴比妥、甲丙酸酯、乙醇和丙戊酸盐产生的中枢神经系统影响不起作用。即使在口服给药后，起效也很快。根据所研究的动物种类，拮抗作用持续时间从几小时到1天不等。ro15 -1788的急性和亚急性毒性很低。未见苯二氮卓类药物的作用。
In neurological and behavioral studies in mice, rats, dogs and squirrel monkeys, the imidazobenzodiazepinone Ro 15-1788 acted as a potent benzodiazepine antagonist. The antagonistic activity was both preventive and curative and seen at doses at which no intrinsic effects were detected. It was highly selective in that it acted against CNS effects induced by benzodiazepines but not against those produced by other depressants, such as phenobarbitone, meprobamate, ethanol and valproate. The onset of action was rapid even after oral administration. Depending on the animal species studied, the antagonistic effects lasted from a few hours to 1 day. The acute and subacute toxicity of Ro 15-1788 was very low. Benzodiazepine-like effects were not seen.