| Literature DB >> 28737885 |
Shahrina Alam1, Kaelyn Skye Lingenfelter1, Aaron M Bender1, Craig W Lindsley1,2,3.
Abstract
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.Entities:
Keywords: 3,5-dimethyladamantan-1-amine hydrochloride; Alzheimer’s disease; Memantine; N-methyl-d-aspartate (NMDA) receptor; glutamatergic dysfunction; uncompetitive antagonist
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Year: 2017 PMID： 28737885 DOI： 10.1021/acschemneuro.7b00270
Source DB: PubMed Journal: ACS Chem Neurosci ISSN： 1948-7193 Impact factor: 4.418