Gmiro V E, Serdyuk S E
Department of Neuropharmacology, Institute of Experimental Medicine, Russian Academy of Medical Sciences, St. Petersburg, Russia.
Bull Exp Biol Med. 2008 Jun;145(6):728-30. doi: 10.1007/s10517-008-0194-3.
Intramuscular injection of selective NMDA receptor antagonists memantine and arcaine 4-fold decreased the incidence of pentylenetetrazole-induced generalized tonic-clonic seizures in rats, while the incidence of clonic seizures decreased by 1.2-1.3 times. Memantine and arcaine are characterized by low therapeutic index, i.e. induced ataxia in rats in doses exceeding the effective anticonvulsant dose by only 3.5-10 times. Intramuscular injection of IEM-1913 (combined blockade of NMDA and AMPA receptors in the brain) decreased the incidence of pentylenetetrazole-induced clonic and tonic-clonic seizures in rats by 4-8 times. The therapeutic index of IEM-1913 surpassed that of memantine and arcaine by 200-600 times.
肌肉注射选择性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂美金刚和阿卡因可使大鼠戊四氮诱导的全身强直阵挛性癫痫发作的发生率降低4倍，而阵挛性癫痫发作的发生率降低1.2 - 1.3倍。美金刚和阿卡因的特点是治疗指数低，即在大鼠中，仅超过有效抗惊厥剂量3.5 - 10倍的剂量就会诱发共济失调。肌肉注射IEM - 1913（联合阻断大脑中的NMDA和AMPA受体）可使大鼠戊四氮诱导的阵挛性和强直阵挛性癫痫发作的发生率降低4 - 8倍。IEM - 1913的治疗指数比美金刚和阿卡因高200 - 600倍。
