Paul S M, Skolnick P
Science. 1978 Nov 24;202(4370):892-4. doi: 10.1126/science.715447.
Seizures induced in the rat by electroshock or by injections of pentylenetetrazol increase the specific binding of diazepam to putative receptor sites in cerebral cortical membranes. The enhancement of diazepam binding results from a rapid increase in the number of available binding sites rather than a change in receptor affinity. The postictal increase in cortical benzodiazepine receptors suggests that the cerebral cortex might be more sensitive to the anticonvulsant effects of the benzodiazepines after seizures. This observation may be related to the mechanism of action of these drugs in the treatment of recurrent seizures such as status epilepticus.
通过电击或注射戊四氮在大鼠中诱发的癫痫发作会增加地西泮与大脑皮质膜中假定受体位点的特异性结合。地西泮结合的增强是由于可用结合位点数量的快速增加,而非受体亲和力的改变。癫痫发作后皮质苯二氮䓬受体的增加表明,癫痫发作后大脑皮质可能对苯二氮䓬类药物的抗惊厥作用更敏感。这一观察结果可能与这些药物治疗癫痫持续状态等复发性癫痫发作的作用机制有关。