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An in vivo evaluation of the antiseizure activity and acute neurotoxicity of agmatine.

机译:胍丁胺的抗癫痫活性和急性神经毒性的体内评估。

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摘要

Agmatine, an endogenous cationic amine, exerts a wide range of biological effects, including modulation of glutamate-activated N-methyl-D-aspartate (NMDA) receptor function in the central nervous system (CNS). Since glutamate and the NMDA receptor have been implicated in the initiation and spread of seizure activity, the capacity of agmatine to inhibit seizure spread was evaluated in vivo. Orally administered agmatine (30 mg/kg) protected against maximal electroshock seizure (MES)-induced seizure spread in rats as rapidly as 15 min and for as long as 6 h after administration. Inhibition of MES-induced seizure spread was also observed when agmatine was administered intraperitoneally. Agmatine's antiseizure activity did not appear to be dose-dependent. An in vivo neurotoxicity screen indicated that agmatine was devoid of any acute neurological toxicity at the doses tested. These preliminary data suggest that agmatine has promising anticonvulsant activity.
机译:胍丁胺是一种内源性阳离子胺,具有多种生物学效应,包括调节中枢神经系统(CNS)中的谷氨酸激活的N-甲基-D-天冬氨酸(NMDA)受体功能。由于谷氨酸和NMDA受体与癫痫发作的发生和传播有关,因此在体内评估了胍丁胺抑制癫痫发作的能力。口服胍丁胺(30 mg / kg)可以防止大鼠遭受最大的电击惊厥(MES)诱发的最大癫痫扩散,最快可在15分钟后持续长达6小时。当腹膜内施用胍丁胺时,也观察到了MES诱导的癫痫发作扩散的抑制。胍丁胺的抗癫痫活性似乎与剂量无关。体内神经毒性筛查表明,胍丁胺在所测试的剂量下没有任何急性神经毒性。这些初步数据表明,胍丁胺具有有希望的抗惊厥活性。

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