BENZODIAZEPINE ANTAGONIST RO 15-1788 - NEUROLOGICAL AND BEHAVIORAL-EFFECTS

被引:347
作者
BONETTI, EP
PIERI, L
CUMIN, R
SCHAFFNER, R
PIERI, M
GAMZU, ER
MULLER, RKM
HAEFELY, W
机构
[1] F HOFFMANN LA ROCHE & CO LTD, DEPT PHARMACEUT RES, CH-4002 BASEL, SWITZERLAND
[2] HOFFMANN LA ROCHE INC, DEPT PHARMACEUT RES, NUTLEY, NJ 07110 USA
关键词
D O I
10.1007/BF00470579
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
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.
引用
收藏
页码:8 / 18
页数:11
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