The low-affinity, use-dependent NMDA receptor antagonist AR-R 15896AR - An update of progress in stroke

被引:12
作者
Palmer, GC [1 ]
Cregan, EF [1 ]
Bialobok, P [1 ]
Sydserff, SG [1 ]
Hudzik, TJ [1 ]
McCarthy, DJ [1 ]
机构
[1] Astra Arcus USA, Rochester, NY 14602 USA
来源
NEUROPROTECTIVE AGENTS: FOURTH INTERNATIONAL CONFERENCE | 1999年 / 890卷
关键词
D O I
10.1111/j.1749-6632.1999.tb08020.x
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Use-dependent N-methyl-D-aspartate (NMDA) receptor antagonists protect neurons from the lethal consequences of excessive stimulation by excitatory amino acids, Clinical development of high-affinity compounds such as MK801 have been limited due to untoward side effects. Toward this end, the lower-affinity use-dependent NMDA antagonists have greater margins of safety and have advanced to clinical trials for stroke, epilepsy, head trauma and chronic neurodegenerative disorders. AR-R 15896AR is currently in Phase II trials for stroke and has been repeatedly demonstrated to afford neuroprotection in a variety of in vivo and in vitro models associated with ischemia/excitotoxic conditions.
引用
收藏
页码:406 / 420
页数:15
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