Articles with "negative allosteric" as a keyword



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Negative allosteric modulators of NMDA receptors with GluN2B subunit: Alanine‐derived benzoxazolone bioisosteres of 2‐methyl‐3‐benzazepine‐1,7‐diols

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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… read more here.

Keywords: nmda receptors; allosteric modulators; moiety; benzoxazolone ... See more keywords
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The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor

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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… read more here.

Keywords: allosteric modulator; negative allosteric; dopamine receptor; pharmacology ... See more keywords
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Negative allosteric modulation of GABAARs at α5 subunit-containing benzodiazepine sites reverses stress-induced anhedonia and weakened synaptic function in mice

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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… read more here.

Keywords: benzodiazepine site; stress; mice; gaba nams ... See more keywords
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Systematic variation of the benzoylhydrazine moiety of the GluN2A selective NMDA receptor antagonist TCN-201.

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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… read more here.

Keywords: tcn 201; nmda receptor; negative allosteric; moiety ... See more keywords
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Subtle modifications to a thieno[2,3-d]pyrimidine scaffold yield negative allosteric modulators and agonists of the dopamine D2 receptor.

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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… read more here.

Keywords: allosteric modulators; thieno pyrimidine; negative allosteric; dopamine receptor ... See more keywords
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Distinctive binding properties of the negative allosteric modulator, [3H]SB269,652, at recombinant dopamine D3 receptors

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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… read more here.

Keywords: allosteric modulator; negative allosteric; dopamine; sb269 652 ... See more keywords
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Antidepressant Effects and Mechanisms of Group II mGlu Receptor-Specific Negative Allosteric Modulators

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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… read more here.

Keywords: mechanisms group; effects mechanisms; negative allosteric; allosteric modulators ... See more keywords
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Identification by virtual screening and functional characterisation of novel positive and negative allosteric modulators of the α7 nicotinic acetylcholine receptor

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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… read more here.

Keywords: positive negative; negative allosteric; nicotinic acetylcholine; allosteric modulators ... See more keywords
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Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABAA Receptor Negative Allosteric Modulators.

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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… read more here.

Keywords: selective gabaa; optimization naphthyridine; derivatives selective; multiparameter optimization ... See more keywords
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Affinity Mass Spectrometry-Based Fragment Screening Identified a New Negative Allosteric Modulator of the Adenosine A2A Receptor Targeting the Sodium Ion Pocket.

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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… read more here.

Keywords: fragment screening; mass spectrometry; affinity mass; negative allosteric ... See more keywords
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Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5

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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… read more here.

Keywords: lead like; glutamate receptor; metabotropic glutamate; allosteric modulators ... See more keywords