Classics in Chemical Neuroscience: Memantine

被引：59

作者：

Alam, Shahrina ^{[1
]}

Lingenfelter, Kaelyn Skye ^{[1
]}

Bender, Aaron M. ^{[1
]}

Lindsley, Craig W. ^{[1
,2
,3
]}

机构：

[1] Vanderbilt Univ, Sch Med, Vanderbilt Ctr Neurosci Drug Discovery, Nashville, TN 37232 USA

[2] Vanderbilt Univ, Sch Med, Dept Pharmacol, Nashville, TN 37232 USA

[3] Vanderbilt Univ, Vanderbilt Inst Chem Biol, Dept Chem, Nashville, TN 37232 USA

来源：

ACS CHEMICAL NEUROSCIENCE | 2017年 / 8卷 / 09期

关键词：

Memantine; 3,5-dimethyladamantan-l-amine hydrochloride; Alzheimer's disease; N-methyl-D-aspartate (NMDA) receptor; uncompetitive antagonist; glutamatergic dysfunction; OBSESSIVE-COMPULSIVE DISORDER; NMDA RECEPTOR ANTAGONISTS; PLACEBO-CONTROLLED TRIAL; ALZHEIMERS-DISEASE; DOUBLE-BLIND; EFFICACY; HYDROCHLORIDE; PHARMACOLOGY; IMPAIRMENT; HYPOTHESIS;

D O I：

10.1021/acschemneuro.7b00270

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Memantine was the first breakthrough medication for the treatment of moderate to severe Alzheimer's disease (AD) patients and represents a fundamentally new mechanism of action (moderate affinity, uncompetitive, voltage-dependent, N-methyl-D-aspartate (NMDA) receptor antagonist that exhibits fast on/off kinetics) to modulate glutamatergic dysfunction. Since its approval by the FDA in 2003, memantine, alone and in combination with donepezil, has improved patient outcomes in terms of cognition, behavioral disturbances, daily functioning, and delaying time to institutionalization. In this review, we will highlight the historical significance of memantine to AD (and other neuropsychiatric disorders) as well as provide an overview of the synthesis, pharmacology, and drug metabolism of this unique NMDA uncompetitive antagonist that clearly secures its place among the Classics in Chemical Neuroscience.

引用

页码：1823 / 1829

页数：7

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