Grecksch G, de Carvalho L P, Venault P, Chapouthier G, Rossier J
Life Sci. 1983 May 30;32(22):2579-84. doi: 10.1016/0024-3205(83)90241-2.
The effects of benzodiazepine antagonist Ro 15-1788, alone or with diazepam, were studied in mice on convulsions induced by pentylenetetrazol (PTZ). We found that Ro 15-1788 (1 mg/kg) was able to antagonize the anticonvulsive effects of diazepam (1 mg/kg), but also had, with submaximal doses of PTZ (65 mg/kg), its own anticonvulsive action. At very low doses (0.1 mg/kg), it even potentiated the anticonvulsive effects of diazepam (0.05 mg/kg). This dual action provides evidence for partial agonist properties of the antagonist Ro 15-1788.
在小鼠中研究了苯二氮䓬拮抗剂Ro 15 - 1788单独使用或与地西泮合用对戊四氮（PTZ）诱导惊厥的影响。我们发现，Ro 15 - 1788（1毫克/千克）能够拮抗地西泮（1毫克/千克）的抗惊厥作用，但在亚最大剂量的PTZ（65毫克/千克）作用下，它自身也具有抗惊厥作用。在非常低的剂量（0.1毫克/千克）时，它甚至增强了地西泮（0.05毫克/千克）的抗惊厥作用。这种双重作用为拮抗剂Ro 15 - 1788的部分激动剂特性提供了证据。
