选择性N-甲基-D-天门冬氨酸受体NR2B亚型阻滞剂近年来受到了越来越多的关注。目前,已报道的NR2B亚型阻滞剂的结构类型绝大多数仍为艾芬地尔发展而来的哌啶衍生物,另外还有酰胺、脒、氨基喹啉等结构类型;NR2B亚型阻滞剂在神经元保护、镇痛、抗药物依赖、抗帕金森病等方面表现了潜力。现根据不同结构类型综述NR2B亚型阻滞剂的结构及药理活性,并探讨其毒副作用较低的可能原因和临床应用潜力。
NR2B subtype selective NMDA receptor antagonists have received considerable attentions in recent years. Currently, most of the NR2B antagonists known are structurally related to ifenprodil, and some belongs to the types of amides, amidines and aminoquinolines. The NR2B antagonists have shown the potential in neuronal protection and prophylaxis of hyperalgesia, drug-dependence and Parkinsong diseases in rodent models. This review presents the correlationship of structure types of the NR2B antagonists with their pharmacological properties together with the rational and clinical therapy of the NR2B antagonists with lower side effects.