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Allosteric antagonist action at triheteromeric NMDA receptors

Gibb, AJ; (2022) Allosteric antagonist action at triheteromeric NMDA receptors. Neuropharmacology , 202 , Article 108861. 10.1016/j.neuropharm.2021.108861. (In press). Green open access

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Abstract

NMDA receptors are one subtype of glutamate receptor that play fundamental roles in synaptic physiology and synaptic plasticity in the nervous system, in addition to being implicated in several neurological disorders. It is now established that many NMDA receptors in the nervous system are triheteromeric, composed of two glycine-binding GluN1 subunits and two different glutamate binding GluN2 subunits. The pharmacology of NMDA receptor has become well established since the pioneering work of Watkins and Evans almost half a century ago and has seen a resurgence of interest in the past decade as new subtype-selective allosteric modulators have been discovered. In this article, features specific to allosteric antagonist action at triheteromeric NMDA receptors are reviewed with a focus on understanding the mechanism of action of drugs acting at triheteromeric GluN1/GluN2B/GluN2D receptors. These receptors are of importance in the basal ganglia and in interneurons of the hippocampus and implications for understanding the action of allosteric antagonists at synaptic triheteromeric receptors are considered.

Type: Article
Title: Allosteric antagonist action at triheteromeric NMDA receptors
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.neuropharm.2021.108861
Publisher version: https://doi.org/10.1016/j.neuropharm.2021.108861
Additional information: © 2021 Published by Elsevier Ltd. This is an open access article under the CC BY 4.0 license Attribution 4.0 International (https://creativecommons.org/licenses/by/4.0/)
Keywords: NMDA receptor, Triheteromeric receptor, Allosteric antagonist
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences > Neuro, Physiology and Pharmacology
URI: https://discovery.ucl.ac.uk/id/eprint/10137778
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