Albertson T E, Bowyer J F, Paule M G
Life Sci. 1982 Oct 11;31(15):1597-601. doi: 10.1016/0024-3205(82)90051-0.
The effects of various doses of diazepam and the new central benzodiazepine antagonist Ro-15-1788 were investigated in fully amygdaloid kindled rats. Diazepam had a pronounced dose-dependent anticonvulsant effect in this model. Ro-15-1788 dose-dependently reduced the behavioral ranks of the elicited kindled seizures to a maximum of 60% of control without consistently modifying the afterdischarge duration. No prestimulation convulsant effects were seen with Ro-15-1788. When 2 mg/kg i.p. of Ro-15-1788 was given after various doses of diazepam, the prestimulation sedation and ataxia anticonvulsant effects of diazepam (0.5-2.0 mg/kg) were attenuated by treatment with 2 mg/kg dose of Ro-15-1788. At the low dose of diazepam (0.25 mg/kg), increased reduction of behavioral rank and after discharge duration was seen after the 2 mg/kg dose of Ro-15-1788. Thus, Ro-15-1788 appears not to have proconvulsant properties in the kindled amygdaloid seizure model. Further, Ro-15-1788 appears to have some anticonvulsant properties of its own. Mixed agonist and antagonist effects were seen with Ro-15-1788 when given after various doses of diazepam in this model.
在完全杏仁核点燃的大鼠中研究了不同剂量地西泮和新型中枢苯二氮䓬拮抗剂Ro-15-1788的作用。在该模型中，地西泮具有明显的剂量依赖性抗惊厥作用。Ro-15-1788剂量依赖性地将诱发的点燃性癫痫发作的行为等级降低至对照的最大60%，而未持续改变放电后持续时间。Ro-15-1788未观察到预刺激惊厥作用。在给予不同剂量地西泮后腹腔注射2mg/kg的Ro-15-1788，地西泮（0.5-2.0mg/kg）的预刺激镇静和共济失调抗惊厥作用因2mg/kg剂量的Ro-15-1788治疗而减弱。在地西泮低剂量（0.25mg/kg）时，2mg/kg剂量的Ro-15-1788后可见行为等级降低和放电后持续时间增加。因此，在点燃的杏仁核癫痫模型中，Ro-15-1788似乎没有促惊厥特性。此外，Ro-15-1788似乎自身具有一些抗惊厥特性。在该模型中，给予不同剂量地西泮后再给予Ro-15-1788时，可见Ro-15-1788具有混合激动剂和拮抗剂作用。
