Jensen L H, Petersen E N, Braestrup C
Life Sci. 1983 Jul 25;33(4):393-9. doi: 10.1016/s0024-3205(83)80014-9.
In experiments with audiogenic seizures in DBA/2 mice, we observed that several socalled benzodiazepine receptor antagonists exhibited either anticonvulsive (Ro 15-1788, PrCC) or proconvulsive (FG 7142, beta-CCE, CGS 8216) effects at high receptor occupancy (17-85%), as compared to benzodiazepines and DMCM which had anticonvulsive and proconvulsive actions, respectively, at very low receptor occupancy (less than 10%). Sensitive distinction between benzodiazepine receptor ligands with low anticonvulsive efficacy (partial agonists) and ligands with low proconvulsive, and maybe anxiogenic, efficacy (partial inverse agonists) can thus be obtained in sound seizure susceptible mice.
在对DBA/2小鼠进行的听源性癫痫发作实验中，我们观察到，与分别在极低受体占有率（低于10%）时具有抗惊厥和惊厥作用的苯二氮䓬类药物及DMCM相比，几种所谓的苯二氮䓬受体拮抗剂在高受体占有率（17 - 85%）时表现出抗惊厥（Ro 15 - 1788、PrCC）或惊厥（FG 7142、β-CCE、CGS 8216）作用。因此，在对声音敏感的癫痫易感小鼠中，可以灵敏地区分抗惊厥效力低的苯二氮䓬受体配体（部分激动剂）和惊厥效力低且可能具有致焦虑作用的配体（部分反向激动剂）。
