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Based on the ability of many receptors to amplify NIH 3T3 cells, we developed a high throughput assay of cloned receptor pharmacology. In this assay, receptors are transiently co-expressed with the marker enzyme beta-galactosidase. Receptors that induce cellular proliferation select and amplify the cells that also express the marker, thus the ability ...
Hans Bräuner‐Osborne, Mark R. Brann
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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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Role for M5 muscarinic acetylcholine receptors in cocaine addiction
Journal of Neuroscience Research, 2003AbstractMuscarinic cholinergic receptors of the M5 subtype are expressed by dopamine‐containing neurons of the ventral tegmentum. These M5 receptors modulate the activity of midbrain dopaminergic neurons, which play an important role in mediating reinforcing properties of abused psychostimulants like cocaine.
Fink-Jensen, A. +11 more
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Discovery of M5 Muscarinic Acetylcholine Receptor Antagonists: 1‐Methyl‐4‐Phenylpiperidine Analogs
Na‐Ra Lee +4 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]
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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Immunological activation of T cells enhances synthesis of acetylcholine (ACh) and transcription of choline acetyltransferase (ChAT), M5 muscarinic ACh receptor (mAChR) and acetylcholinesterase (AChE). Stimulation of mAChRs on T and B cells causes oscillating Ca(2+)-signaling and up-regulation of c-fos expression; moreover, M1 mAChRs play a crucial role
Yoshihito X. Fujii +9 more
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The Muscarinic Acetylcholine Receptor M 5 : Therapeutic Implications and Allosteric Modulation
ACS Chemical Neuroscience, 2018The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) was the most recent mAChR to be cloned and has since emerged as a potential therapeutic target for a number of indications. Early studies with knockout animals have provided clues to the receptor's role in physiological processes related to Alzheimer's disease, schizophrenia, and addiction ...
Aaron M. Bender +2 more
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The neuromuscular blocking drug alcuronium was found earlier to increase the affinity of muscarinic receptors for methyl-N-scopolamine (NMS). This effect could be observed in some but not in other tissues. Subtype selectivity of the positive allosteric action of alcuronium was now investigated in radioligand binding experiments in Chinese hamster ovary
Ján Jakubík +3 more
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Isolation and Functional Characterization of the Chick M5 Muscarinic Acetylcholine Receptor Gene
Journal of Neurochemistry, 2000Abstract: 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.
S, Creason, K M, Tietje, N M, Nathanson
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