Results 231 to 240 of about 29,153 (282)

Characterising the M1 muscarinic acetylcholine receptor in the gastrointestinal tract.

2023
The M1 receptor is a protein found in the brain and is heavily implicated in memory and cognition. Drugs targeted at this protein can also cause diarrhoea, but the precise mechanism of this gastrointestinal effect is unknown. This thesis aimed to understand how the M1 receptor affects gastrointestinal function by using compounds that specifically ...
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Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline.

ACS Chemical Neuroscience, 2018
Preclinical and clinical data suggest that muscarinic acetylcholine receptor activation may be therapeutically beneficial for the treatment of schizophrenia and Alzheimer's diseases.
C. Thorn, Joshua Moon, Clinton A Bourbonais, J. Harms, J. Edgerton, Eda Stark, Stefanus J. Steyn, Christopher R Butter, J. Lazzaro, Rebecca E O'connor, M. Popiolek   +10 more
semanticscholar   +1 more source

Excitatory effect of M1 muscarinic acetylcholine receptor on automaticity of mouse heart

Archives of Pharmacal Research, 2005
We have investigated the effects of relatively high concentration of carbachol (CCh), an agonist of muscarinic acetylcholine receptor (mAChR), on cardiac automaticity in mouse heart. Action potentials from automatically beating right atria of mice were measured with conventional microelectrodes.
Kwang-II Kwon, Chin Ok Lee, Sun-Hee Woo, Byung Ho Lee   +3 more
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Targeting the M1 muscarinic acetylcholine receptor in neurodegeneration

2023
Alzheimer’s disease (AD) is the most common neurodegenerative disorder, and to date, no disease-modifying treatments exist. The M1 muscarinic acetylcholine receptor (mAChR) is an established therapeutic target for the symptomatic treatment of AD, and drugs activating the M1 mAChR have been shown to improve cognitive decline and behavioural symptoms in ...
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Scanning Mutagenesis Studies of the M 1 Muscarinic Acetylcholine Receptor

Receptors and Channels, 2003
Following the solution of the structure of bovine rhodopsin by X-ray crystallography, it has been possible to build an improved homology model of the M(1) muscarinic acetylcholine receptor. This has been used to interpret the outcome of an extensive series of scanning and point mutagenesis studies on the transmembrane domain of the receptor.
M. S. Bee, Edward C. Hulme, Zhi-Liang Lu
openaire   +3 more sources

Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.

Journal of Medicinal Chemistry, 2022
The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) represents a novel potential target for the treatment of multiple addictive disorders, including opioid use disorder.
Aaron T Garrison, Douglas L. Orsi, Rory A. Capstick, David Whomble, Jinming Li, Trever R. Carter, Andrew S. Felts, P. Vinson, Alice L. Rodriguez, Allie Han, Krishma Hajari, Hyekyung P. Cho, Laura B. Teal, Madeline G Ragland, M. Ghamari-Langroudi, M. Bubser, Sichen Chang, N. Schnetz-Boutaud, O. Boutaud, Anna L Blobaum, Daniel J. Foster, C. Niswender, P. Conn, C. Lindsley, Carrie K Jones, Changho Han   +25 more
semanticscholar   +1 more source

Selective cognitive dysfunction in acetylcholine M1 muscarinic receptor mutant mice

Nature Neuroscience, 2002
Blockade of cholinergic neurotransmission by muscarinic receptor antagonists produces profound deficits in attention and memory. However, the antagonists used in previous studies bind to more than one of the five muscarinic receptor subtypes. Here we examined memory in mice with a null mutation of the gene coding the M1 receptor, the most densely ...
Geoffrey G. Murphy, Nancy P. Rahnama, Susan E. Hamilton, Neil M. Nathanson, Scott L. Mitchell, Stephan G. Anagnostaras, Alcino J. Silva   +6 more
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Effects of anandamide on the binding and signaling properties of M1 muscarinic acetylcholine receptors

Biochemical Pharmacology, 2004
This study investigated the effects of the endocannabinoid, anandamide, on M(1) muscarinic acetylcholine receptors (mAChRs) expressed in Chinese hamster ovary (CHO) cells. In the presence of anandamide, [(3)H]N-methylscopolamine ([(3)H]NMS) inhibition binding was characterized by Hill coefficients greater than 1 while saturation binding isotherms were ...
Arthur Christopoulos, Alfred Lanzafame, Elizabeth Guida   +2 more
openaire   +3 more sources

Toward activated homology models of the human M1 muscarinic acetylcholine receptor

Journal of Molecular Graphics and Modelling, 2014
Structure-based virtual screening offers a good opportunity for the discovery of selective M1 muscarinic acetylcholine receptor (mAChR) agonists for the treatment of Alzheimer's disease. However, no 3-D structure of an M1 mAChR is yet available and the homology models that have been previously reported are only able to identify antagonists in virtual ...
Stephen W. Doughty, David K. Chalmers, Michael J. C. Buckle, Elizabeth Yuriev, Sek Peng Chin   +4 more
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Scanning mutagenesis of transmembrane domain 3 of the m1 muscarinic acetylcholine receptor

Journal of Physiology-Paris, 1998
Scanning mutagenesis of transmembrane domain 3 of the M1 muscarinic acetylcholine receptor has revealed a highly-differentiated alpha-helical structure. Lipid-facing residues are distinguished from a patch of residues which selectively stabilise the ground state of the receptor, and from a band of amino acids extending the full length of the helix ...
Zhi-Liang Lu, Edward C. Hulme
openaire   +3 more sources