Gareri Pietro, Condorelli Daniele, Belluardo Natale, Russo Emilio, Loiacono Antonella, Barresi Vincenza, Trovato-Salinaro Angela, Mirone Melita B, Ferreri Ibbadu Guido, De Sarro Giovambattista
Section of Pharmacology, Department of Experimental and Clinical Medicine, Faculty of Medicine and Surgery, University of Catanzaro, 88100 Catanzaro, Italy.
Neuropharmacology. 2004 Dec;47(8):1205-16. doi: 10.1016/j.neuropharm.2004.08.021.
Carbenoxolone (CBX), the succinyl ester of glycyrrhetinic acid, is an inhibitor of gap junctional intercellular communication. Systemic administration of CBX was able to decrease the seizure severity score and to increase the latency time of seizure onset in genetically epilepsy prone rats (GEPRs). In particular, intravenous or intraperitoneal administration of carbenoxolone (5-30 mg/kg) produced a dose-dependent and significant reduction in the clonic and tonic phases of the audiogenic seizures in GEPRs. The anticonvulsant doses were not associated with an impairment of motor coordination. The bilateral microinjection of CBX (0.001-0.50 microg/0.5 microl) into the inferior colliculi, the substantia nigra (pars reticulata or compacta) and the inferior olivary complex was able to reduce the seizure severity score in a dose-dependent manner. The anticonvulsant effects were longer lasting after focal microinjection than after systemic administration. No anticonvulsant effects were observed following focal bilateral microinjections of glycyrrhizin into the same brain areas where CBX was shown to be effective.
甘草次酸琥珀酸酯即生胃酮（CBX），是一种缝隙连接细胞间通讯的抑制剂。对遗传性癫痫易感大鼠（GEPRs）进行生胃酮的全身给药，能够降低癫痫发作严重程度评分，并延长癫痫发作起始的潜伏时间。具体而言，静脉注射或腹腔注射生胃酮（5 - 30毫克/千克）可使GEPRs听源性癫痫的阵挛期和强直期出现剂量依赖性的显著缩短。抗惊厥剂量与运动协调性受损无关。向下丘、黑质（网状部或致密部）和下橄榄核复合体双侧微量注射生胃酮（0.001 - 0.50微克/0.5微升）能够剂量依赖性地降低癫痫发作严重程度评分。局部微量注射后的抗惊厥作用比全身给药后的持续时间更长。在与显示生胃酮有效的相同脑区进行双侧局部微量注射甘草甜素后，未观察到抗惊厥作用。
