Abstract
Glutamatergic neurotransmission, of special importance in the human brain, is implicated in key brain functions such as synaptic plasticity and memory. The excessive activation of N-methyl- D-aspartate (NMDA) receptors may result in excitotoxic neuronal damage; this process has been implicated in the pathomechanism of different neurodegenerative disorders, such as Alzheimer’s disease (AD). Memantine is an uncompetitive antagonist of NMDA receptors with a favorable pharmacokinetic profile, and is therefore clinically well tolerated. Memantine is approved for the treatment of AD, but may additionally be beneficial for other dementia forms and pain conditions. Kynurenic acid (KYNA) is an endogenous antagonist of NMDA receptors which has been demonstrated under experimental conditions to be neuroprotective. The development of a well-tolerated NMDA antagonist may offer a novel therapeutic option for the treatment of neurodegenerative disease and pain syndromes. KYNA may be a valuable candidate for future drug development.
Keywords: Dementia, glutamate, kynurenic acid, memantine, neuroprotection, NMDA.
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Current Neuropharmacology
Title:Memantine and Kynurenic Acid: Current Neuropharmacological Aspects
Volume: 14 Issue: 2
Author(s): Zsófia Majláth, Nóra Török, József Toldi and László Vécsei
Affiliation:
Keywords: Dementia, glutamate, kynurenic acid, memantine, neuroprotection, NMDA.
Abstract: Glutamatergic neurotransmission, of special importance in the human brain, is implicated in key brain functions such as synaptic plasticity and memory. The excessive activation of N-methyl- D-aspartate (NMDA) receptors may result in excitotoxic neuronal damage; this process has been implicated in the pathomechanism of different neurodegenerative disorders, such as Alzheimer’s disease (AD). Memantine is an uncompetitive antagonist of NMDA receptors with a favorable pharmacokinetic profile, and is therefore clinically well tolerated. Memantine is approved for the treatment of AD, but may additionally be beneficial for other dementia forms and pain conditions. Kynurenic acid (KYNA) is an endogenous antagonist of NMDA receptors which has been demonstrated under experimental conditions to be neuroprotective. The development of a well-tolerated NMDA antagonist may offer a novel therapeutic option for the treatment of neurodegenerative disease and pain syndromes. KYNA may be a valuable candidate for future drug development.
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Cite this article as:
Majláth Zsófia, Török Nóra, Toldi József and Vécsei László, Memantine and Kynurenic Acid: Current Neuropharmacological Aspects, Current Neuropharmacology 2016; 14 (2) . https://dx.doi.org/10.2174/1570159X14666151113123221
DOI https://dx.doi.org/10.2174/1570159X14666151113123221 |
Print ISSN 1570-159X |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6190 |
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