Search Results - "Hellyer, Shane D"
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Unlocking the secrets of trace amine-associated receptor 1 agonists: new horizon in neuropsychiatric treatment
Published in Frontiers in psychiatry (31-10-2024)“…For over seven decades, dopamine receptor 2 (D 2 receptor) antagonists remained the mainstay treatment for neuropsychiatric disorders. Although it is effective…”
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Trace amine associated receptor 1: predicted effects of single nucleotide variants on structure-function in geographically diverse populations
Published in Human genomics (11-06-2024)“…Trace Amine Associated Receptor 1 (TAAR1) is a novel pharmaceutical target under investigation for the treatment of several neuropsychiatric conditions. TAAR1…”
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SCA44‐ and SCAR13‐associated GRM1 mutations affect metabotropic glutamate receptor 1 function through distinct mechanisms
Published in British journal of pharmacology (01-11-2024)“…Background and Purpose Metabotropic glutamate receptor 1 (mGlu1) is a promising therapeutic target for neurodegenerative CNS disorders including…”
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Rigorous Characterization of Allosteric Modulation of the Human Metabotropic Glutamate Receptor 1 Reveals Probe- and Assay-Dependent Pharmacology
Published in Molecular pharmacology (01-06-2023)“…Allosteric modulation of metabotropic glutamate receptor subtype 1 (mGlu ) represents a viable therapeutic target for treating numerous central nervous system…”
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Metabotropic glutamate receptor 5 (mGlu5)‐positive allosteric modulators differentially induce or potentiate desensitization of mGlu5 signaling in recombinant cells and neurons
Published in Journal of neurochemistry (01-11-2019)“…Allosteric modulators of metabotropic glutamate receptor 5 (mGlu5) are a promising therapeutic strategy for a number of neurological disorders. Multiple…”
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Probe dependence and biased potentiation of metabotropic glutamate receptor 5 is mediated by differential ligand interactions in the common allosteric binding site
Published in Biochemical pharmacology (01-07-2020)“…[Display omitted] The metabotropic glutamate receptor 5 (mGlu5) is a promising therapeutic target for multiple CNS disorders. Recent mGlu5 drug discovery has…”
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Differential contribution of metabotropic glutamate receptor 5 common allosteric binding site residues to biased allosteric agonism
Published in Biochemical pharmacology (01-07-2020)“…[Display omitted] Allosteric modulators of metabotropic glutamate receptor subtype 5 (mGlu5) represent an attractive therapeutic strategy for multiple CNS…”
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Metabotropic glutamate receptor 5 (mGlu 5 )-positive allosteric modulators differentially induce or potentiate desensitization of mGlu 5 signaling in recombinant cells and neurons
Published in Journal of neurochemistry (01-11-2019)“…Allosteric modulators of metabotropic glutamate receptor 5 (mGlu ) are a promising therapeutic strategy for a number of neurological disorders. Multiple mGlu…”
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9
Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology
Published in Neuropharmacology (01-05-2019)“…Allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGlu5) have been proposed as potential therapies for various CNS disorders. These…”
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10
Adenosine receptor signalling in Alzheimer’s disease
Published in Purinergic signalling (01-09-2022)“…Alzheimer’s disease (AD) is the most common dementia in the elderly and its increasing prevalence presents treatment challenges. Despite a better understanding…”
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Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias
Published in Molecular pharmacology (01-05-2021)“…Positive allosteric modulation of metabotropic glutamate subtype 5 (mGlu ) receptor has emerged as a potential new therapeutic strategy for the treatment of…”
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12
Publisher Correction to: Adenosine receptor signalling in Alzheimer’s disease
Published in Purinergic signalling (01-12-2022)Get full text
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13
Identification of monellin as the first naturally derived proteinaceous allosteric agonist of metabotropic glutamate receptor 5
Published in Basic & clinical pharmacology & toxicology (01-06-2020)“…Allosteric modulators bind sites distinct from orthosteric ligands, allowing for improved spatiotemporal control of receptors and greater subtype selectivity…”
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Development of Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 2 Based on Two Positive Allosteric Modulator Chemotypes
Published in ACS chemical neuroscience (03-06-2020)“…The metabotropic glutamate receptor 2 (mGlu ) is a transmembrane-spanning class C G protein-coupled receptor that is an attractive therapeutic target for…”
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15
Pinnatoxins E, F and G target multiple nicotinic receptor subtypes
Published in Journal of neurochemistry (01-11-2015)“…Pinnatoxins are members of the cyclic imine group of marine phycotoxins that are highly toxic in in vivo rodent bioassays, causing rapid death due to…”
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Neuromuscular blocking activity of pinnatoxins E, F and G
Published in Toxicon (Oxford) (15-12-2013)“…Pinnatoxins are produced by dinoflagellates and belong to the cyclic imine family of toxins. They are fast-acting and highly toxic when administered in vivo in…”
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Marine algal pinnatoxins E and F cause neuromuscular block in an in vitro hemidiaphragm preparation
Published in Toxicon (Oxford) (01-12-2011)“…Members of the cyclic imine group of toxins, gymnodimine and spirolides, have been found to be potent antagonists of both muscle type and neuronal nicotinic…”
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In vitro labelling of muscle type nicotinic receptors using a fluorophore-conjugated pinnatoxin F derivative
Published in Toxicon (Oxford) (01-09-2014)“…Fluorescent molecules are regularly utilised to study ligand–receptor interactions. Many ligands for nicotinic receptors have been conjugated with fluorophores…”
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T54. INVESTIGATING TRANSCRIPTOMIC PROFILE AND NEURITE OUTGROWTH IN ADHD USING INDUCED PLURIPOTENT STEM CELLS DIFFERENTIATED INTO DOPAMINE NEURONS
Published in European neuropsychopharmacology (01-10-2024)“…Attention deficit hyperactivity disorder (ADHD) is the most prevalent neurodevelopmental condition globally. It is characterized by inattention,…”
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Pharmacology, Signaling and Therapeutic Potential of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators
Published in ACS pharmacology & translational science (05-11-2024)Get full text
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