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Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200177
Abstract: Inspired by besonprodil, the phenol of potent negative allosteric modulators of GluN2B‐N‐methyl‐d‐aspartate (NMDA) receptors was replaced by a benzoxazolone system. To increase the similarity to the lead compounds, an additional methyl moiety was installed in…
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Keywords:
nmda receptors;
allosteric modulators;
moiety;
benzoxazolone ... See more keywords
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Published in 2018 at "Biochemical Pharmacology"
DOI: 10.1016/j.bcp.2018.01.002
Abstract: Graphical abstract Figure. No caption available. ABSTRACT SB269652 is a negative allosteric modulator of the dopamine D2 receptor (D2R) yet possesses structural similarity to ligands with a competitive mode of interaction. In this study, we…
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Keywords:
allosteric modulator;
negative allosteric;
dopamine receptor;
pharmacology ... See more keywords
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Published in 2021 at "Biological psychiatry"
DOI: 10.1016/j.biopsych.2021.11.024
Abstract: BACKGROUND Abnormal reward processing, typically anhedonia, is a hallmark of human depression and is accompanied by altered functional connectivity in reward circuits. Negative allosteric modulators of GABAA (gamma-aminobutyric acid A) receptors (GABA-NAMs) have rapid antidepressant-like…
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Keywords:
benzodiazepine site;
stress;
mice;
gaba nams ... See more keywords
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Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.09.006
Abstract: GluN2A containing N-methyl-D-aspartate receptors (NMDARs) are important ion channels in the central nervous system and highly involved in several different neurophysiological but also neuropathophysiological processes. However, current understanding of the contribution of GluN2A containing NMDARs…
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Keywords:
tcn 201;
nmda receptor;
negative allosteric;
moiety ... See more keywords
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Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.01.061
Abstract: We recently described a structurally novel series of negative allosteric modulators (NAMs) of the dopamine D2 receptor (D2R) based on thieno[2,3-d]pyrimidine 1, showing it can be structurally simplified to reveal low molecular weight, fragment-like NAMs…
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Keywords:
allosteric modulators;
thieno pyrimidine;
negative allosteric;
dopamine receptor ... See more keywords
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Published in 2018 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2017.12.002
Abstract: ABSTRACT Recently, employing radioligand displacement and functional coupling studies, we demonstrated that SB269,652 (N‐[(1r,4r)−4‐[2‐(7‐cyano‐1,2,3,4‐tetrahydroisoquinolin‐2‐yl)ethyl]cyclohexyl]−1H‐indole‐2‐carboxamide) interacts in an atypical manner with dopamine D3 receptor displaying a unique profile reminiscent of a negative allosteric ligand. Here, we…
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Keywords:
allosteric modulator;
negative allosteric;
dopamine;
sb269 652 ... See more keywords
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Published in 2020 at "Neuron"
DOI: 10.1016/j.neuron.2019.12.011
Abstract: In this issue of Neuron, Joffe et al. (2020) assess the antidepressant-relevant effects and underlying neural mechanisms of negative allosteric modulators selective for either metabotropic glutamate receptors 2 (mGlu2) or 3 (mGlu3). Negative modulation of both…
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Keywords:
mechanisms group;
effects mechanisms;
negative allosteric;
allosteric modulators ... See more keywords
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Published in 2018 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2018.07.009
Abstract: ABSTRACT Several previous studies have demonstrated that the activity of neurotransmitters acting on ligand‐gated ion channels such as the nicotinic acetylcholine receptor (nAChR) can be altered by compounds binding to allosteric modulatory sites. In the…
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Keywords:
positive negative;
negative allosteric;
nicotinic acetylcholine;
allosteric modulators ... See more keywords
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Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00414
Abstract: The discovery and characterization of novel naphthyridine derivatives with selective α5-GABAAR negative allosteric modulator (NAM) activity are disclosed. Utilizing a scaffold-hopping strategy, fused [6 + 6] bicyclic scaffolds were designed and synthesized. Among these, 1,6-naphthyridinones…
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Keywords:
selective gabaa;
optimization naphthyridine;
derivatives selective;
multiparameter optimization ... See more keywords
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Published in 2021 at "ACS chemical biology"
DOI: 10.1021/acschembio.0c00899
Abstract: Allosteric ligands provide new opportunities to modulate G protein-coupled receptor (GPCR) function and present therapeutic benefits over orthosteric molecules. Negative allosteric modulators (NAMs) can inhibit the activation of a receptor and downstream signal transduction. Screening…
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Keywords:
fragment screening;
mass spectrometry;
affinity mass;
negative allosteric ... See more keywords
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Published in 2022 at "ACS Chemical Biology"
DOI: 10.1021/acschembio.2c00234
Abstract: Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed the location of allosteric binding sites and opened new opportunities for the discovery of novel modulators. In this work, molecular docking screens for allosteric…
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Keywords:
lead like;
glutamate receptor;
metabotropic glutamate;
allosteric modulators ... See more keywords