Abstract
A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit nanomolar potency is unusual, and the underlying SAR is detailed.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Allosteric Regulation
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Drug Design*
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Inhibitory Concentration 50
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Ligands
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Molecular Structure
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Protein Binding / drug effects
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Receptor, Metabotropic Glutamate 5
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Receptors, Metabotropic Glutamate / metabolism*
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Small Molecule Libraries / chemical synthesis*
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Small Molecule Libraries / chemistry
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Small Molecule Libraries / pharmacology
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Structure-Activity Relationship
Substances
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Ligands
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Receptor, Metabotropic Glutamate 5
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Receptors, Metabotropic Glutamate
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Small Molecule Libraries