Tyurenkov I N, Borodkina L E, Bagmetova V V, Berestovitskaya V M, Vasil'eva O S
Volgograd State Medical University, Volgograd, Russia.
A. I. Herzen State Pedagogical University of Russia, St. Petersburg, Russia.
Bull Exp Biol Med. 2016 Feb;160(4):465-9. doi: 10.1007/s10517-016-3198-4. Epub 2016 Feb 23.
GABA analogs containing phenyl (phenibut) or para-chlorophenyl (baclofen) substituents demonstrated nootropic activity in a dose of 20 mg/kg: they improved passive avoidance conditioning, decelerated its natural extinction, and exerted antiamnestic effect on the models of amnesia provoked by scopolamine or electroshock. Tolyl-containing GABA analog (tolibut, 20 mg/kg) exhibited antiamnestic activity only on the model of electroshock-induced amnesia. Baclofen and, to a lesser extent, tolibut alleviated seizures provoked by electroshock, i.e. both agents exerted anticonvulsant effect. All examined GABA aryl derivatives demonstrated neuroprotective properties on the maximum electroshock model: they shortened the duration of coma and shortened the period of spontaneous motor activity recovery. In addition, these agents decreased the severity of passive avoidance amnesia and behavioral deficit in the open field test in rats exposed to electroshock. The greatest neuroprotective properties were exhibited by phenyl-containing GABA analog phenibut.
含有苯基（苯乙胺）或对氯苯基（巴氯芬）取代基的GABA类似物在剂量为20mg/kg时表现出益智活性：它们改善了被动回避条件反射，减缓了其自然消退，并对由东莨菪碱或电击诱发的失忆模型产生抗失忆作用。含甲苯基的GABA类似物（托利布，20mg/kg）仅在电击诱发失忆模型上表现出抗失忆活性。巴氯芬以及程度较轻的托利布减轻了电击诱发的癫痫发作，即两种药物均发挥了抗惊厥作用。所有检测的GABA芳基衍生物在最大电击模型上均表现出神经保护特性：它们缩短了昏迷持续时间，并缩短了自发运动活动恢复的时间。此外，这些药物降低了电击大鼠在旷场试验中被动回避失忆和行为缺陷的严重程度。含苯基的GABA类似物苯乙胺表现出最大的神经保护特性。
