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N-甲基-D-天冬氨酸(NMDA)受体拮抗剂在衰老相关疾病中的潜在应用及当前使用情况。

Potential and current use of N-methyl-D-aspartate (NMDA) receptor antagonists in diseases of aging.

作者信息

Le D A, Lipton S A

机构信息

Stroke and Neurovascular Regulation Laboratory, Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts, USA.

出版信息

Drugs Aging. 2001;18(10):717-24. doi: 10.2165/00002512-200118100-00001.

Abstract

The N-methyl-D-aspartate (NMDA) receptor complex is a subtype of glutamate receptor and its dysfunction is involved in many neurological disorders associated with aging, including chronic pain, depression, stroke and Parkinson's disease. Multiple clinical trials using NMDA receptor antagonists have been aborted mainly due to the severe psychomimetic adverse effects of these drugs that occur before concentrations can reach an adequate level in the brain. In this review, we present the evidence that clinically safer NMDA antagonists such as memantine and nitroglycerin, and the combination drug nitro-memantine, are promising as drugs in treating neurodegenerative diseases.

摘要

N-甲基-D-天冬氨酸(NMDA)受体复合物是谷氨酸受体的一种亚型,其功能障碍与许多与衰老相关的神经疾病有关,包括慢性疼痛、抑郁症、中风和帕金森病。多项使用NMDA受体拮抗剂的临床试验已中止,主要是因为这些药物在大脑中达到足够浓度之前就会出现严重的拟精神病副作用。在这篇综述中,我们提供证据表明,临床上更安全的NMDA拮抗剂,如美金刚和硝酸甘油,以及联合药物硝基美金刚,有望成为治疗神经退行性疾病的药物。

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