Booker J G, Dailey J W, Jobe P C, Lane J D
Life Sci. 1986 Sep 1;39(9):799-806. doi: 10.1016/0024-3205(86)90458-3.
Adult male and female genetically seizure-prone rats were assessed for sound-induced seizures. Heterozygous control groups were compared with mild seizure (designated GEPR 3) and severe seizure animals (GEPR 9). Groups of animals were killed and crude synaptosome fractions (P2) prepared from freshly dissected cerebral cortices. Binding sites for gamma-aminobutyric acid (GABA) were assessed by [3H]-muscimol in the absence or presence of excess GABA and/or pentobarbital. Binding sites for benzodiazepines were assessed by [3H]-flunitrazepam in the presence or absence of clonazepam. Compared to controls, GEPR 3 animals had a modest increase and GEPR 9 animals a larger increase in Bmax for both high and low affinity GABA sites, with no change in Kd. Chloride-dependent, barbiturate-enhanced GABA binding (increased Bmax) was observed in all conditions and groups. Likewise benzodiazepine binding (Bmax) increased slightly in GEPR 9 animals. There were no observed changes in binding sites for a survey of biogenic amines. Seizure-prone animals appear to have compensatory denervation-like supersensitivity for their most prominent inhibitory receptor, which may or may not be linked to the seizure event.
对成年雄性和雌性遗传性癫痫易感大鼠进行声音诱发癫痫的评估。将杂合对照组与轻度癫痫发作组（命名为GEPR 3）和重度癫痫发作组（GEPR 9）进行比较。处死动物组，并从新鲜解剖的大脑皮质制备粗制突触体组分（P2）。在存在或不存在过量γ-氨基丁酸（GABA）和/或戊巴比妥的情况下，用[³H] - 蝇蕈醇评估GABA的结合位点。在存在或不存在氯硝西泮的情况下，用[³H] - 氟硝西泮评估苯二氮䓬类药物的结合位点。与对照组相比，GEPR 3动物的高亲和力和低亲和力GABA位点的Bmax适度增加，GEPR 9动物的增加幅度更大，而Kd没有变化。在所有条件和组中均观察到氯离子依赖性、巴比妥酸盐增强的GABA结合（Bmax增加）。同样，GEPR 9动物中的苯二氮䓬类药物结合（Bmax）略有增加。对生物胺的一项调查显示，结合位点没有观察到变化。癫痫易感动物似乎对其最主要的抑制性受体具有代偿性去神经样超敏反应，这可能与癫痫发作事件有关，也可能无关。
