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Recent progress in allosteric modulators for GluN2A subunit and development of GluN2A-selective nuclear imaging probes


He, Yingfang; Mu, Linjing; Ametamey, Simon M; Schibli, Roger (2019). Recent progress in allosteric modulators for GluN2A subunit and development of GluN2A-selective nuclear imaging probes. Journal of Labelled Compounds and Radiopharmaceuticals, 62(8):552-560.

Abstract

N-methyl-D-aspartate (NMDA) receptors play key roles in physiology by regulating the synaptic plasticity and the cellular mechanism involved in learning and memory. The GluN2A subunit is the most abundant expression of NMDA receptors in mature brain, and its dysfunction has been implicated in various neurological disorders. However, the function of GluN2A subunit in physiological and pathological conditions is not yet completely unveil due to the lack of subunit-selective ligands, including specific positron emission tomography (PET)/single photon emission computed tomography (SPECT) imaging probes. In this review, recent progresses in understanding its pathophysiological role, the structure-activity relationship, and the postulated mechanisms of novel GluN2A ligands as well as status of molecular imaging probes for PET are summarized.

Abstract

N-methyl-D-aspartate (NMDA) receptors play key roles in physiology by regulating the synaptic plasticity and the cellular mechanism involved in learning and memory. The GluN2A subunit is the most abundant expression of NMDA receptors in mature brain, and its dysfunction has been implicated in various neurological disorders. However, the function of GluN2A subunit in physiological and pathological conditions is not yet completely unveil due to the lack of subunit-selective ligands, including specific positron emission tomography (PET)/single photon emission computed tomography (SPECT) imaging probes. In this review, recent progresses in understanding its pathophysiological role, the structure-activity relationship, and the postulated mechanisms of novel GluN2A ligands as well as status of molecular imaging probes for PET are summarized.

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Additional indexing

Item Type:Journal Article, refereed, further contribution
Communities & Collections:04 Faculty of Medicine > University Hospital Zurich > Clinic for Nuclear Medicine
Dewey Decimal Classification:610 Medicine & health
Scopus Subject Areas:Physical Sciences > Analytical Chemistry
Life Sciences > Biochemistry
Health Sciences > Radiology, Nuclear Medicine and Imaging
Life Sciences > Drug Discovery
Physical Sciences > Spectroscopy
Physical Sciences > Organic Chemistry
Language:English
Date:30 June 2019
Deposited On:05 Feb 2020 18:44
Last Modified:29 Jul 2020 13:08
Publisher:Wiley-Blackwell Publishing, Inc.
ISSN:0362-4803
OA Status:Closed
Publisher DOI:https://doi.org/10.1002/jlcr.3744
PubMed ID:31037756

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