Results 1 to 10 of about 18,227 (256)

Weight Gain With Advancing Age Is Controlled by the Muscarinic Acetylcholine Receptor M4 in Male Mice.

Endocrinology
Obesity is characterized by the excessive accumulation of adipose tissue, and it is a serious global health issue. Understanding the pathology of obesity is crucial for developing effective interventions.
Takahashi T, Takase Y, Shiraishi A, Matsubara S, Watanabe T, Kirimoto S, Yamagaki T, Osawa M.   +7 more
europepmc   +5 more sources

The muscarinic M4 acetylcholine receptor exacerbates symptoms of movement disorders [PDF]

Biochemical Society Transactions, 2023
Barbeau's seesaw hypothesis of dopamine-acetylcholine balance has predominated movement disorders literature for years. Both the simplicity of the explanation and the matching efficacy of anticholinergic treatment in movement disorders seem to support ...
Nicole Chambers, Michael Millett, Mark S. Moehle   +2 more
semanticscholar   +4 more sources

Structure-activity relationship of pyrazol-4-yl-pyridine derivatives and identification of a radiofluorinated probe for imaging the muscarinic acetylcholine receptor M₄. [PDF]

Acta Pharm Sin B, 2023
Haider A, Deng X, Mastromihalis O, Pfister SK, Jeppesen TE, Xiao Z, Pham V, Sun S, Rong J, Zhao C, Chen J, Li Y, Connors TR, Davenport AT, Daunais JB, Hosseini V, Ran W, Christopoulos A, Wang L, Valant C, Liang SH.   +20 more
europepmc   +3 more sources

[¹¹C]MK-6884 PET imaging reveals lower M₄ muscarinic acetylcholine receptor availability following cocaine self-administration in male rats. [PDF]

Pharmacol Rep
Background Cocaine Use Disorder (CUD) remains a significant problem in the United States, with high rates of relapse and no present FDA-approved treatment.
Gollapelli KK, Krizan I, Bhoopal B, Damuka N, Moriarty C, Miller M, Sai KKS, Gould RW.   +7 more
europepmc   +3 more sources

Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres [PDF]

ACS Medicinal Chemistry Letters, 2019
It has been hypothesized that selective muscarinic acetylcholine receptor (mAChR) M4 subtype activation could provide therapeutic benefits to a number of neurological disorders while minimizing unwanted cholinergic side effects observed due to ...
Qingyi Yang, Erik LaChapelle, Natasha M. Kablaoui, Damien Webb, Michael Popiolek, Sarah Grimwood, Rouba Kozak, Rebecca E. O’Connor, John T. Lazzaro, Christopher R. Butler, Lei Zhang   +10 more
semanticscholar   +5 more sources

Identification, expression and functional characterization of M4L, a muscarinic acetylcholine M4 receptor splice variant. [PDF]

PLoS ONE, 2017
Rodent genomic alignment sequences support a 2-exon model for muscarinic M4 receptor. Using this model a novel N-terminal extension was discovered in the human muscarinic acetylcholine M4 receptor. An open reading frame was discovered in the human, mouse
Douglas A Schober, Carrie H Croy, Cara L Ruble, Ran Tao, Christian C Felder   +4 more
doaj   +6 more sources

The potential of muscarinic M1 and M4 receptor activators for the treatment of cognitive impairment associated with schizophrenia [PDF]

Frontiers in Psychiatry
Cognitive impairment is a core symptom of schizophrenia and a major determinant of poor long-term functional outcomes. Despite considerable efforts, we do not yet have any approved pharmacological treatments for cognitive impairment associated with ...
Samantha E. Yohn, Phillip D. Harvey, Stephen K. Brannan, William P. Horan, William P. Horan   +4 more
doaj   +3 more sources

New Tricks for an Old Dog: Biased GPCR Agonism of an M4 Muscarinic Acetylcholine Receptor Antagonist in Airway Smooth Muscle Cells

American Journal of Respiratory Cell and Molecular Biology, 2022
ligands, the expectation is that they will only trigger G-protein–independent pathways that promote antiremodeling and bronchorelaxant actions via b -arrestin pathways that are distinct from those driving bronchial hyperresponsiveness.
Yassine Amrani
openalex   +3 more sources

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

eLife, 2023
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level understanding of the general principles that govern the myriad pharmacological effects exerted by GPCR ...
Ziva Vuckovic, Jinan Wang, Vi Pham, Jesse I Mobbs, Matthew J Belousoff, Apurba Bhattarai, Wessel AC Burger, Geoff Thompson, Mahmuda Yeasmin, Vindhya Nawaratne, Katie Leach, Emma T van der Westhuizen, Elham Khajehali, Yi-Lynn Liang, Alisa Glukhova, Denise Wootten, Craig W Lindsley, Andrew Tobin, Patrick Sexton, Radostin Danev, Celine Valant, Yinglong Miao, Arthur Christopoulos, David M Thal   +23 more
doaj   +2 more sources

Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4) [PDF]

Journal of biomolecular screening, 2015
Muscarinic acetylcholine receptors (mAChRs) have long been viewed as viable targets for novel therapeutic agents for the treatment of Alzheimer’s disease and other disorders involving impaired cognitive function. In an attempt to identify orthosteric and
Emery Smith, Peter Chase, Colleen M. Niswender, Thomas J. Utley, Douglas J. Sheffler, Meredith J. Noetzel, Atin Lamsal, Michael R. Wood, P. Jeffrey Conn, Craig W. Lindsley, Franck Madoux, Mary Acosta, Louis Scampavia, Timothy Spicer, Peter Hodder   +14 more
openalex   +2 more sources