Pérez C, Otero Losada M E, Rubio M C
Gen Pharmacol. 1985;16(6):629-32. doi: 10.1016/0306-3623(85)90156-9.
Male Wistar rats were chronically treated with 2 mg/kg per day bicuculline i.p. during 10 days. Biochemical parameters related to the GABAergic system in CNS were analyzed. A 63% increase in glutamic acid decarboxylase activity was found in treated animals. Endogenous GABA levels were not modified. The treatment increased Bmax of GABA binding by 112% without changing the KD value. The treatment decreased Bmax of diazepam binding by 40% whereas it did not change the KD value. Diazepam binding was enhanced by in vitro addition of GABA at the same extent as in treated animals.
雄性Wistar大鼠连续10天每天腹腔注射2mg/kg荷包牡丹碱进行慢性处理。分析了与中枢神经系统中γ-氨基丁酸（GABA）能系统相关的生化参数。在接受处理的动物中发现谷氨酸脱羧酶活性增加了63%。内源性GABA水平未改变。该处理使GABA结合的最大结合容量（Bmax）增加了112%，而解离常数（KD）值未改变。该处理使地西泮结合的Bmax降低了40%，而KD值未改变。在体外添加GABA后，地西泮结合增强的程度与处理动物相同。
