申请人:State of Oregon
公开号:US05262568A1
公开(公告)日:1993-11-16
Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
三取代和四取代的胍基化合物,对苯环异氰酸酯(PCP)受体具有高结合亲和力,且更倾向于对脑内sigma受体具有低亲和力。这些胍基衍生物作为NMDA受体的非竞争性抑制剂,通过作用于NMDA受体离子通道复合物的阻滞剂,从而阻止谷氨酸诱导的NMDA受体反应。这些化合物因此具有神经保护作用,并可用于治疗缺氧、低血糖、脑或脊髓缺血、脑或脊髓创伤以及癫痫、阿尔茨海默病、肌萎缩性侧索硬化症、帕金森病、亨廷顿病、唐氏综合征、科萨科夫病和其他神经退行性疾病的治疗。