Bonetti E P, Pieri L, Cumin R, Schaffner R, Pieri M, Gamzu E R, Müller R K, Haefely W
Psychopharmacology (Berl). 1982;78(1):8-18. doi: 10.1007/BF00470579.
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 found to be very low. Benzodiazepine-like effects were not seen.
在对小鼠、大鼠、狗和松鼠猴进行的神经学和行为学研究中，咪唑并苯二氮䓬酮Ro 15 - 1788表现为一种强效的苯二氮䓬拮抗剂。其拮抗活性兼具预防性和治疗性，且在未检测到内在效应的剂量下即可显现。它具有高度选择性，即它能对抗苯二氮䓬类药物诱导的中枢神经系统效应，但对其他抑制剂（如苯巴比妥、甲丙氨酯、乙醇和丙戊酸盐）产生的效应则无作用。即使口服给药后，起效也很快。根据所研究的动物种类不同，拮抗作用持续数小时至1天。结果发现Ro 15 - 1788的急性和亚急性毒性非常低。未观察到类似苯二氮䓬的效应。
