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N-甲基-D-天冬氨酸(NMDA)受体相关开放通道阻滞剂美金刚在新生大鼠局灶性脑缺血光血栓形成模型中的神经保护作用

Neuroprotection by the NMDA receptor-associated open-channel blocker memantine in a photothrombotic model of cerebral focal ischemia in neonatal rat.

作者信息

Stieg P E, Sathi S, Warach S, Le D A, Lipton S A

机构信息

CNS Research Institute, Neurosurgical Service, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.

出版信息

Eur J Pharmacol. 1999 Jun 30;375(1-3):115-20. doi: 10.1016/s0014-2999(99)00214-9.

Abstract

Excessive accumulation of glutamate or other excitatory amino acids and the subsequent overactivity of NMDA receptors is currently thought to lead to neuronal injury in cerebral ischemia. Therefore, antagonists of the NMDA receptor may offer an approach for the treatment of ischemic brain injury. Dizocilpine (MK-801), an NMDA receptor-associated channel blocker, protects neurons in several rodent stroke models. However, this drug has numerous side effects and causes apoptosis of neonatal neurons. Recently, another NMDA receptor-associated channel blocker, memantine, has been shown to ameliorate NMDA-receptor mediated neurotoxicity in neuronal cell cultures and in focal cerebral ischemia models in adult rats without substantial side effects. Memantine has been used clinically in the treatment of Parkinson's disease and spasticity for a number of years. Here we tested the effects of memantine on focal stroke caused by photochemical thrombosis in neonatal rats and demonstrated a neuroprotective effect of memantine in this model. We also found excellent correlation between infarct size determined by magnetic resonance imaging (MRI) and histopathological analysis in the same animals. A single pre-ischemic dose of memantine (20 mg/kg) given 15 min prior to induction of stroke reduced the infarct size by 36.3% when compared to control animals treated with normal saline (P < 0.0001). At this dosage, memantine manifests few, if any, neurobehavioral side effects. Thus memantine appears to be both safe and effective in neonatal as well as adult animal models of stroke.

摘要

目前认为,谷氨酸或其他兴奋性氨基酸的过度积累以及随后NMDA受体的过度激活会导致脑缺血中的神经元损伤。因此,NMDA受体拮抗剂可能为缺血性脑损伤的治疗提供一种方法。地佐环平(MK-801)是一种与NMDA受体相关的通道阻滞剂,在几种啮齿动物中风模型中可保护神经元。然而,这种药物有许多副作用,并会导致新生神经元凋亡。最近,另一种与NMDA受体相关的通道阻滞剂美金刚已被证明可改善神经元细胞培养物和成年大鼠局灶性脑缺血模型中NMDA受体介导的神经毒性,且无明显副作用。美金刚已在临床上用于治疗帕金森病和痉挛多年。在此,我们测试了美金刚对新生大鼠光化学血栓形成所致局灶性中风的影响,并在该模型中证明了美金刚的神经保护作用。我们还发现,在同一动物中,磁共振成像(MRI)测定的梗死面积与组织病理学分析之间具有良好的相关性。在诱导中风前15分钟给予单次缺血前剂量的美金刚(20 mg/kg),与用生理盐水治疗的对照动物相比,梗死面积减少了36.3%(P < 0.0001)。在此剂量下,美金刚几乎没有神经行为副作用。因此,美金刚在新生动物和成年动物中风模型中似乎都是安全有效的。

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