Results 241 to 250 of about 29,153 (282)

On the Unique Binding and Activating Properties of Xanomeline at the M1 Muscarinic Acetylcholine Receptor

Molecular Pharmacology, 1998
We investigated the molecular nature of the interaction between the functionally selective M1 muscarinic acetylcholine receptor (mAChR) agonist xanomeline and the human M1 mAChR expressed in Chinese hamster ovary (CHO) cells. In contrast to the non-subtype-selective agonist carbachol, xanomeline demonstrated M1 mAChR binding that was resistant to ...
A, Christopoulos, T L, Pierce, J L, Sorman, E E, El-Fakahany   +3 more
openaire   +2 more sources

Targeting the muscarinic M1 receptor with a selective, brain-penetrant antagonist to promote remyelination in multiple sclerosis

Proceedings of the National Academy of Sciences of the United States of America
Significance Multiple sclerosis is a chronic and debilitating neurological disease that results in inflammatory demyelination and neuronal loss. Mechanisms that promote remyelination are being considered as promising therapeutic approaches.
Michael M Poon, Kymmy Lorrain, K. Stebbins, Geraldine C Edu, A. Broadhead, Ariana J Lorenzana, Jeffrey R. Roppe, Jill M Baccei, C. Baccei, Austin Chen, Ari J. Green, D. Lorrain, Jonah R Chan   +12 more
semanticscholar   +1 more source

Characterization of methanthelinium binding and function at human M1–M5 muscarinic acetylcholine receptors [PDF]

Naunyn-Schmiedeberg's Archives of Pharmacology, 2018
Firstly, it was determined whether methanthelinium bromide (MB) binds to human M1-M5 (hM1-hM5) muscarinic acetylcholine receptors in comparison to the classical muscarinic antagonist N-methylscopolamine (NMS). [3H]NMS dissociation binding experiments revealed an allosteric retardation of dissociation at 100 μM of MB ranging from none in hM3 to 4.6-fold
Matthias Irmen, Janine Holze, Theresa Bödefeld, Christian Tränkle   +3 more
openaire   +2 more sources

Interaction of anandamide with the M1 and M4 muscarinic acetylcholine receptors

Brain Research, 2001
The M(1) and M(4) muscarinic acetylcholine receptors are the most abundant muscarinic receptor subtypes in the brain, and are involved in learning and memory. Because cannabinoid receptors are also abundantly expressed in similar brain regions and mediate opposite effects to acetylcholine on cognition, the present study investigated whether the ...
Arthur Christopoulos, Kathryn M Wilson
openaire   +3 more sources

Differential Regulation of the M1 Muscarinic Acetylcholine Receptor by Orthosteric and Allosteric Ligands

The FASEB Journal, 2008
AC‐42 (4‐n‐butyl‐1‐[4‐(2‐methylphenyl)‐4‐oxo‐1‐butyl] piperidine hydrogen chloride) is a selective M1 muscarinic receptor agonist with an allosteric mechanism of action. Here, we have investigated whether AC‐42 and two orthosteric muscarinic agonists (oxotremorine‐M (oxo‐M) and pilocarpine) cause internalization and down‐regulation of the M1 muscarinic
Rachel L. Thomas, Martyn D. Wood, John Challiss, Christopher J. Langmead   +3 more
openaire   +2 more sources

In Silico Study in MPO and Molecular Docking of the Synthetic Drynaran Analogues Against the Chronic Tinnitus: Modulation of the M1 Muscarinic Acetylcholine Receptor

Molecular Biotechnology, 2023
M. N. da Rocha, Aluísio Marques da Fonseca, Adriana Nogueira Machado Dantas, H. S. dos Santos, E. S. Marinho, G. S. Marinho   +5 more
semanticscholar   +1 more source

Behavioral effects of morphine and cocaine in M1 muscarinic acetylcholine receptor-deficient mice

Psychopharmacology, 2007
Muscarinic acetylcholine receptors (M1-M5) modulate the activity of the central nervous system and an array of physiological functions. Recent evidence has also implicated muscarinic receptors in behavioral effects of drugs of abuse such as morphine and cocaine.
Kelly A. Carrigan, Linda A. Dykstra
openaire   +3 more sources

Disrupted tonotopy of the auditory cortex in mice lacking M1 muscarinic acetylcholine receptor

Hearing Research, 2005
Sensory cortices have multiple and distinct functional maps that systematically represent environmental information. Development of these maps is precisely controlled by a number of intrinsic and extrinsic factors. Cortical cholinergic regulation is a crucial factor for normal cortical morphogenesis. In this study, we test the role of the M1 muscarinic
Yunfeng Zhang, Richard H. Dyck, Susan E. Hamilton, Neil M. Nathanson, Jun Yan   +4 more
openaire   +3 more sources

M1 muscarinic acetylcholine receptor interacts with BACE1 and regulates its proteosomal degradation

Neuroscience Letters, 2012
A prime culprit in the pathogenesis of Alzheimer's disease (AD) is overproduction/aggregation of β-amyloid (Aβ), which is derived from β-Amyloid Precursor Protein through sequential cleavages by β-site APP cleaving protein 1 (BACE1) and γ-secretase. The level/activity of BACE1 is elevated in sporadic AD and identification of proteins that affect BACE1 ...
Jiang, Shangtong, Wang, Yan, Ma, Qilin, Zhou, Aina, Zhang, Xian, Zhang, Yun-wu   +5 more
openaire   +4 more sources

M1 is a major subtype of muscarinic acetylcholine receptors on mouse colonic epithelial cells

Journal of Gastroenterology, 2012
Muscarinic acetylcholine receptors (mAChRs) are major regulators of gut epithelial functions. However, the precise subtype composition has not been clarified.We characterized the pharmacological profile of mAChRs on mouse colonic crypts, employing [(3)H]-N-methyl scopolamine chloride as a radioligand and several subtype-selective chemicals, and the ...
Abu Syed Md Anisuzzaman, Hisayoshi Hayashi, Hiroki Ikeuchi, Tomoko Takano, Motoi Uchino, Takanobu Taniguchi, Ikunobu Muramatsu, Rafiqul Islam Khan, Yanju Ma, Yanju Ma, Junsuke Uwada, Fumitaka Ushikubi, Shingo Semba, Atsuo Maemoto, Yuichi Suzuki   +14 more
openaire   +3 more sources