Enhancing NMDA Receptor Function: Recent Progress on Allosteric Modulators

The N-methyl-D-aspartate receptors (NMDARs) are subtype glutamate receptors that play important roles in excitatory neurotransmission and synaptic plasticity. Their hypo- or hyperactivation are proposed to contribute to the genesis or progression of various brain diseases, including stroke, schizoph...

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Main Authors: Lulu Yao, Qiang Zhou
Format: Article
Language:English
Published: Wiley 2017-01-01
Series:Neural Plasticity
Online Access:http://dx.doi.org/10.1155/2017/2875904
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author Lulu Yao
Qiang Zhou
author_facet Lulu Yao
Qiang Zhou
author_sort Lulu Yao
collection DOAJ
description The N-methyl-D-aspartate receptors (NMDARs) are subtype glutamate receptors that play important roles in excitatory neurotransmission and synaptic plasticity. Their hypo- or hyperactivation are proposed to contribute to the genesis or progression of various brain diseases, including stroke, schizophrenia, depression, and Alzheimer’s disease. Past efforts in targeting NMDARs for therapeutic intervention have largely been on inhibitors of NMDARs. In light of the discovery of NMDAR hypofunction in psychiatric disorders and perhaps Alzheimer’s disease, efforts in boosting NMDAR activity/functions have surged in recent years. In this review, we will focus on enhancing NMDAR functions, especially on the recent progress in the generation of subunit-selective, allosteric positive modulators (PAMs) of NMDARs. We shall also discuss the usefulness of these newly developed NMDAR-PAMs.
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spelling doaj-art-0ad957920a0f47bb9c3bac2d1c5a53882025-02-03T06:06:00ZengWileyNeural Plasticity2090-59041687-54432017-01-01201710.1155/2017/28759042875904Enhancing NMDA Receptor Function: Recent Progress on Allosteric ModulatorsLulu Yao0Qiang Zhou1School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, ChinaSchool of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, ChinaThe N-methyl-D-aspartate receptors (NMDARs) are subtype glutamate receptors that play important roles in excitatory neurotransmission and synaptic plasticity. Their hypo- or hyperactivation are proposed to contribute to the genesis or progression of various brain diseases, including stroke, schizophrenia, depression, and Alzheimer’s disease. Past efforts in targeting NMDARs for therapeutic intervention have largely been on inhibitors of NMDARs. In light of the discovery of NMDAR hypofunction in psychiatric disorders and perhaps Alzheimer’s disease, efforts in boosting NMDAR activity/functions have surged in recent years. In this review, we will focus on enhancing NMDAR functions, especially on the recent progress in the generation of subunit-selective, allosteric positive modulators (PAMs) of NMDARs. We shall also discuss the usefulness of these newly developed NMDAR-PAMs.http://dx.doi.org/10.1155/2017/2875904
spellingShingle Lulu Yao
Qiang Zhou
Enhancing NMDA Receptor Function: Recent Progress on Allosteric Modulators
Neural Plasticity
title Enhancing NMDA Receptor Function: Recent Progress on Allosteric Modulators
title_full Enhancing NMDA Receptor Function: Recent Progress on Allosteric Modulators
title_fullStr Enhancing NMDA Receptor Function: Recent Progress on Allosteric Modulators
title_full_unstemmed Enhancing NMDA Receptor Function: Recent Progress on Allosteric Modulators
title_short Enhancing NMDA Receptor Function: Recent Progress on Allosteric Modulators
title_sort enhancing nmda receptor function recent progress on allosteric modulators
url http://dx.doi.org/10.1155/2017/2875904
work_keys_str_mv AT luluyao enhancingnmdareceptorfunctionrecentprogressonallostericmodulators
AT qiangzhou enhancingnmdareceptorfunctionrecentprogressonallostericmodulators