Memantine (hydrochloride)

一种NMDA受体拮抗剂；浓度为12μM时可阻断大鼠视网膜神经节细胞中NMDA诱导的电流90%；体外逆转I1PP2A诱导的tau194-207去磷酸化的抑制；2mg/kg时可恢复PP2A活性，降低海马、大脑皮层和脑室区域的GSK-3β和Aβ水平，并减弱阿尔茨海默病AAV1-I1PP2A大鼠模型的空间学习和记忆能力；20mg/kg时可降低大鼠在线索诱导的乙醇寻找测试中对乙醇相关杠杆的反应；在局灶性脑缺血小鼠模型中，可减少MMP-9的分泌、胶原蛋白IV的降解、脑缺血引起的脑梗塞的大小以及神经元细胞死亡。An NMDA receptor antagonist; blocks NMDA-induced currents in rat retinal ganglion cells by 90% at 12 μM; reverses I1PP2A-induced inhibition of dephosphorylation of tau194-207 in vitro; restores PP2A activity, decreases GSK-3β and Aβ levels in the hippocampus, cerebral cortex, and ventricular areas, and attenuates spatial learning and memory in the AAV1-I1PP2A rat model of Alzheimer's disease at 2 mg/kg; reduces responding on the ethanol-associated lever in a cue-induced ethanol seeking test in rats at 20 mg/kg; decreases secretion of MMP-9, degradation of collagen IV, the size of cerebral ischemia-induced brain infarcts, and neuronal cell death in a mouse model of focal cerebral ischemia.