Activation mechanism of the M5 muscarinic acetylcholine receptor
Lee Roy+3 more
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Muscarinic Acetylcholine Receptor M5 Involved in Spermatogenesis through the Modification of Cell-Cell Junctions [PDF]
Abstract The authors have withdrawn this preprint due to author disagreement.
Yong Zhao+8 more
+5 more sources
Expression of muscarinic acetylcholine receptors M3 and M5 in osteoporosis [PDF]
Cholinergic signaling via muscarinic acetylcholine receptors (mAChR) is known to influence various physiological functions. In bone, M3 mAChR and M5 mAChR were identified on the membrane of osteoblast-like cells. M3 mAChR seems to be particularly relevant for bone physiology, as signaling via this receptor was reported to increase bone formation and ...
Reinhard Schnettler
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Isolation and Functional Characterization of the Chick M5 Muscarinic Acetylcholine Receptor Gene [PDF]
Abstract: The chick is a widely used system for study of the actions of muscarinic acetylcholine receptors in the cardiovascular, visual, and nervous systems. We report the isolation and functional analysis of the gene encoding the chick M5 muscarinic receptor.
Sharon A. Creason+2 more
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The membrane signaling properties of the neuronal type-5 muscarinic acetylcholine receptor (M5 AChR) as expressed in murine L cells were studied. Recipient Ltk- cells responded to ATP acting through a P2-purinergic receptor by increasing phosphoinositide hydrolysis 2-fold but were unresponsive to 17 receptor agonists that are stimulatory in other cells.
C F Liao+3 more
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All muscarinic acetylcholine receptors (M1-M5) are expressed in murine brain microvascular endothelium [PDF]
AbstractClinical and experimental studies indicate that muscarinic acetylcholine receptors are potential pharmacological targets for the treatment of neurological diseases. Although these receptors have been described in human, bovine and rat cerebral microvascular tissue, a subtype functional characterization in mouse brain endothelium is lacking ...
Beatrice Mihaela Radu+13 more
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Downstream Signaling of Muscarinic M<sub>4</sub> Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]
ABSTRACT 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
europepmc +2 more sources
Microscopic Binding of M5 Muscarinic Acetylcholine Receptor with Antagonists by Homology Modeling, Molecular Docking, and Molecular Dynamics Simulation [PDF]
By performing homology modeling, molecular docking, and molecular dynamics (MD) simulations, we have developed three-dimensional (3D) structural models of the M5 muscarinic acetylcholine receptor (mAChR) and two complexes for M5 mAChR binding with antagonists SVT-40776 and solifenacin in the environment of lipid bilayer and solvent water.
Xiaoqin Huang+2 more
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Carbachol‐induced reverse transformation of Chinese hamster ovary cells transfected with and expressing the m5 muscarinic acetylcholine receptor [PDF]
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
openalex +5 more sources
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]
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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