Carbachol‐induced reverse transformation of Chinese hamster ovary cells transfected with and expressing the m5 muscarinic acetylcholine receptor [PDF]
FEBS Letters, 1989 Reverse transformation was induced in Chinese hamster ovary (CHO) cells transfected with and stably expressing the m5 subtype of the muscarinic acetylcholine receptor when stimulated with the muscarinic agonist, carbachol. Atropine, a muscarinic antagonist, blocked the carbachol‐stimulated reverse transformation.
Christian C. Felder +2 more
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Muscarinic—but Not Nicotinic—Acetylcholine Receptors Mediate a Nitric Oxide-Dependent Dilation in Brain Cortical Arterioles: A Possible Role for the M5 Receptor Subtype [PDF]
Journal of Cerebral Blood Flow & Metabolism, 2000 Increases in cortical cerebral blood flow are induced by stimulation of basal forebrain cholinergic neurons. This response is mediated in part by nitric oxide (NO) and reportedly involves both nicotinic and muscarinic receptors, some of which are possibly located in the vessel wall.
Ahmed Elhusseiny, Édith Hamel
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Neuropharmacology, 2023 Recent evidence suggests that inhibition of the M5 muscarinic acetylcholine receptor (mAChR) may provide a novel non-opioid mechanism for the treatment of opioid use disorder (OUD). Previous studies from our group and others have demonstrated that acute administration of the long-acting M5 negative allosteric modulator (NAM) ML375 attenuates ...
Laura B. Teal +5 more
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Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-Trifluoromethoxy N-Benzyl Isatins [PDF]
Journal of Medicinal Chemistry, 2009 This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS, identified VU0119498, which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca(2+) mobilization assays ...
Thomas M. Bridges +9 more
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Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M1 – M5 muscarinic acetylcholine receptors [PDF]
Bioorganic & Medicinal Chemistry Letters, 2018 Novel quinuclidinyl N-phenylcarbamate analogs were synthesized, and binding affinities at M1-M5 muscarinic acetylcholine receptor (mAChR) subtypes were determined using Chinese hamster ovary (CHO) cell membranes stably expressing one specific subtype of human mAChR. Although not subtype selective, the lead analog (±)-quinuclidin-3-yl-(4-fluorophenethyl)
Nara Lee +5 more
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Activation mechanism of the M5 muscarinic acetylcholine receptor
Biophysical Journal, 2023 Lee Roy +3 more
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Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, 2010 Besides some pharmacological, biochemical and biophysical evidences support the contention that muscarinic acetylcholine receptors can form homo- and heterodimers, the existence of specific M3 and M5 muscarinic receptors oligomers in living cells is a new concept.
Dasiel O. Borroto‐Escuela +4 more
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P2‐207: Discovery of a highly M5‐preferring muscarinic acetylcholine receptor allosteric potentiator [PDF]
Alzheimer's & Dementia, 2009 Thomas M. Bridges +6 more
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Downstream Signaling of Muscarinic M<sub>4</sub> Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]
Pharmacol Res PerspectABSTRACT Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators. Considering the importance of comprehending M4 receptor pharmacology for these therapeutic applications, this study investigates M4 receptor ...
Merz M +5 more
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Frontiers in Cellular Neuroscience, 2021 The dopamine transporter (DAT) clears neurotransmitters from the extracellular space and serves as an important regulator of signal amplitude and duration at sites of dopamine release. Several different intracellular signaling pathways have been observed
Suzanne M. Underhill, Susan G. Amara
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