Identification of a Novel Delta Opioid Receptor Agonist Chemotype with Potential Negative Allosteric Modulator Capabilities [PDF]
Molecules, 2021 The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed.
Yazan J. Meqbil +7 more
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Evidence for Two Modes of Binding of the Negative Allosteric Modulator SB269,652 to the Dopamine D2 Receptor [PDF]
Biomedicines, 2021 SB269,652 has been described as the first negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), however, the binding mode and allosteric mechanism of action of this ligand remain incompletely understood.
Richard Ågren, Kristoffer Sahlholm
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Amyloid Beta Peptide Is an Endogenous Negative Allosteric Modulator of Leptin Receptor [PDF]
Neuroendocrinology, 2020 Introduction: Metabolic dysfunction is now recognized as a pivotal component of Alzheimer’s disease (AD), the most common dementia worldwide. However, the precise molecular mechanisms linking metabolic dysfunction to AD remain elusive.
E. Cecon +11 more
semanticscholar +4 more sources
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder [PDF]
ACS Medicinal Chemistry Letters, 2018 Lawrence R Marcin +2 more
exaly +3 more sources
Cannabidiphorol (CBDP) acts as a negative allosteric modulator at two distinct sites of cannabinoid receptor 1 [PDF]
Communications ChemistryWhile Δ9-tetrahydrocannabinol (THC) offers significant pain relief, its psychoactive side effects limit its clinical utility. The discovery of cannabidiol (CBD) as a negative allosteric modulator (NAM) of cannabinoid receptor 1 (CB1R) establishes ...
Pankaj Pandey +7 more
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Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells [PDF]
Nature CommunicationsA promising drug target, SETDB1, is a dual methyl-lysine (Kme) reader and methyltransferase implicated in cancer and neurodegenerative disease progression.
Mélanie Uguen +25 more
doaj +2 more sources
Partial mGlu5 Negative Allosteric Modulator M-5MPEP Demonstrates Antidepressant-Like Effects on Sleep Without Affecting Cognition or Quantitative EEG [PDF]
Frontiers in Neuroscience, 2021 Selective negative allosteric modulators (NAMs) targeting the metabotropic glutamate receptor subtype 5 (mGlu5) demonstrate anxiolytic-like and antidepressant-like effects yet concern regarding adverse effect liability remains.
Kimberly M. Holter +11 more
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Allosteric Modulation of Muscarinic Acetylcholine Receptors
Pharmaceuticals, 2010 An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.
Esam E. El-Fakahany, Jan Jakubík
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The metabotropic glutamate receptor 5 negative allosteric modulator fenobam: pharmacokinetics, side effects, and analgesic effects in healthy human subjects. [PDF]
Pain, 2020 Metabotropic glutamate receptor 5 (mGlu5) has been shown to modulate nociception in animals, but no mGlu5 antagonists have been developed commercially as analgesics.
Cavallone LF +8 more
europepmc +2 more sources
Sodium functions as a negative allosteric modulator of the oxytocin receptor.
Biochimica et Biophysica Acta (BBA) - Biomembranes, 2018 The oxytocin receptor, a class A G protein coupled receptor (GPCR), is essentially involved in the physiology of reproduction. Two parameters are crucially important to support high-affinity agonist binding of the receptor: Mg2+ and cholesterol, both ...
Andrea Schiffmann, G. Gimpl
semanticscholar +3 more sources