Wenk G L, Zajaczkowski W, Danysz W
Arizona Research Laboratories, Department of Psychology, University of Arizona, Tucson, USA.
Behav Brain Res. 1997 Feb;83(1-2):129-33. doi: 10.1016/s0166-4328(97)86056-1.
The present study investigated whether chronic, low dose therapy with memantine could (1) prevent the loss of basal forebrain cholinergic cells induced by injection of N-methyl-D-aspartate (NMDA) into the nucleus basalis magnocellularis (NBM) of rats, and (2) attenuate impaired performance in the radial maze of rats with entorhinal cortex lesions. In addition, we investigated whether neuroprotection could be provided by neurokinin B (NKB). Following an injection of NMDA (0.015 M) into the NBM, rats were implanted with osmotic minipumps containing memantine (20 or 0.20 mg/kg/day for 2 weeks). Other rats were given unilateral NBM injections of 1.0 microliter of Solution A (0.5 microliter containing 8.26 mM NKB and 0.24 units of bacitracin and 0.5 microliter containing 0.03 M NMDA) or Solution B (0.5 microliter of PBS containing 0.24 U of bacitracin and 0.5 microliter containing 0.03 M NMDA). Two weeks later, the anterior cortex was analyzed for choline acetyltransferase (ChAT), a specific marker for the loss of acetylcholinergic neurons. Both chronic administration of memantine, and acute administration of NKB, prevented the decline in cortical ChAT activity associated with injection of NMDA into the NBM, and attenuated a reference memory deficit in the radial maze produced by entorhinal cortex lesions. Thus, memantine infusion at low doses leading to steady-state serum levels within a therapeutic range provides both neuroprotection and cognitive enhancement-an optimal combination for the treatment of neurodegenerative disorders.
(1)预防因向大鼠基底大细胞核(NBM)注射N-甲基-D-天冬氨酸(NMDA)所诱导的基底前脑胆碱能细胞丢失;(2)减轻伴有内嗅皮层损伤的大鼠在放射状迷宫实验中受损的行为表现。此外,我们还研究了神经激肽B(NKB)是否能提供神经保护作用。向NBM注射NMDA(0.015 M)后,给大鼠植入含有美金刚的渗透微型泵(20或0.20 mg/kg/天,持续2周)。其他大鼠接受单侧NBM注射1.0微升溶液A(0.5微升含8.26 mM NKB和0.24单位杆菌肽,0.5微升含0.03 M NMDA)或溶液B(0.5微升含0.24 U杆菌肽的PBS和0.5微升含0.03 M NMDA)。两周后,分析前皮质中的胆碱乙酰转移酶(ChAT),这是乙酰胆碱能神经元丢失的特异性标志物。美金刚的慢性给药以及NKB的急性给药均能预防与向NBM注射NMDA相关的皮质ChAT活性下降,并减轻由内嗅皮层损伤导致的放射状迷宫实验中的参考记忆缺陷。因此,低剂量输注美金刚使血清水平在治疗范围内达到稳态,可提供神经保护和认知增强作用——这是治疗神经退行性疾病的最佳组合。