Results 1 to 10 of about 18,462 (237)

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

Acta Pharmaceutica Sinica B, 2023
There is an accumulating body of evidence implicating the muscarinic acetylcholine receptor 4 (M4) in schizophrenia and dementia with Lewy bodies, however, a clinically validated M4 positron emission tomography (PET) radioligand is currently lacking.
Ahmed Haider, Xiaoyun Deng, Olivia Mastromihalis, Stefanie K. Pfister, Troels E. Jeppesen, Zhiwei Xiao, Vi Pham, Shaofa Sun, Jian Rong, Chunyu Zhao, Jiahui Chen, Yinlong Li, Theresa R. Connors, April T. Davenport, James B. Daunais, Vahid Hosseini, Wenqing Ran, Arthur Christopoulos, Lu Wang, Celine Valant, Steven H. Liang   +20 more
doaj   +4 more sources

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

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   +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
Cocaine Use Disorder (CUD) remains a significant problem in the United States, with high rates of relapse and no present FDA-approved treatment. The acetylcholine neurotransmitter system, specifically through modulation of muscarinic acetylcholine ...
Gollapelli KK, Krizan I, Bhoopal B, Damuka N, Moriarty C, Miller M, Sai KKS, Gould RW.   +7 more
europepmc   +4 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

Monoamine Oxidase Inhibition by Major Tanshinones from Salvia miltiorrhiza and Selective Muscarinic Acetylcholine M4 Receptor Antagonism by Tanshinone I [PDF]

Biomolecules, 2021
Monoamine oxidases (MAOs) and muscarinic acetylcholine receptors (mAChRs) are considered important therapeutic targets for Parkinson’s disease (PD). Lipophilic tanshinones are major phytoconstituents in the dried roots of Salvia miltiorrhiza that have ...
Ritu Prajapati, Se Eun Park, Su Hui Seong, Pradeep Paudel, Fazlin Mohd Fauzi, Hyun Ah Jung, Jae Sue Choi   +6 more
openalex   +2 more sources

Xanomeline/trospium-induced polyuria: A patient case report [PDF]

Mental Health Clinician
Xanomeline/trospium is a newly approved agent for the management of schizophrenia. Unlike traditional antipsychotics, which are D2 receptor antagonists, xanomeline is an M1/M4 muscarinic acetylcholine receptor agonist coformulated with trospium, a ...
Henry Leach, PharmD, BCPP, Francesca DiGuglielmo, PharmD   +1 more
doaj   +2 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   +3 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
openalex   +2 more sources

Involvement of Cyclin Dependent Kinase 5 in M4 Muscarinic Acetylcholine Receptor-Mediated Cholinergic Transmission within the Mouse Dorsal Striatum [PDF]

, 2021
Background: An imbalance between dopamine (DA) and acetylcholine (ACh) within the striatum has reemerged as key to the pathophysiology of the neurodegenerative disorder, Parkinson's disease (PD). M4 is a prominent muscarinic ACh receptor subtype in the
Hu Zhou, Huaxiang Shi, Xing Li, Jingxin Zhang, Xin Sui, Zhe Zhao, Zhiyong Nie, Yongan Wang, Jin Li, Liyun Wang   +9 more
openalex   +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