Results 201 to 210 of about 18,462 (237)

The M1 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) VU0453595 and M4 PAM VU0467154 Normalize Sleep‐Wake Architecture Deficits in Aged Mice

Alzheimer's & Dementia, 2022
Declining basal forebrain cholinergic integrity has been associated with disturbances in sleep‐wake architecture in Alzheimer’s Disease (AD). Acetylcholinesterase inhibitors (AChEIs) provide symptomatic treatment for the cognitive deficits in AD through ...
Jason K. Russell, M. Bubser, Shalonda M. Ingram, P. Newhouse, C. Lindsley, Carrie K Jones   +5 more
semanticscholar   +1 more source

Development of Novel M4 Muscarinic Acetylcholine Receptor Antagonists for the Treatment of Movement Disorders

The FASEB Journal, 2022
Non‐selective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some movement disorders, including Parkinson’s disease and dystonia.
Jerri L. Rook, Aaron M. Bender, J. Dickerson, Daniel J Foster, Alice L. Rodriguez, C. Niswender, E. Hess, J. Conn, C. Lindsley   +8 more
semanticscholar   +1 more source

Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.

Journal of Medicinal Chemistry
Selective activation of the M4 muscarinic acetylcholine receptor subtype offers a novel strategy for the treatment of psychosis in multiple neurological disorders.
Christopher R Butler, M. Popiolek, Laura A McAllister, Erik A. Lachapelle, Melissa Kramer, Elizabeth M Beck, S. Mente, M. Brodney, Matthew Brown, Adam M. Gilbert, Chris Helal, Kevin Ogilvie, Jeremy Starr, Daniel Uccello, Sarah Grimwood, Jeremy R. Edgerton, Jonathan Garst-Orozko, Rouba Kozak, Susan Lotarski, A. Rossi, Deborah Smith, Rebecca O’Connor, J. Lazzaro, C. Steppan, Stefanus J. Steyn   +24 more
semanticscholar   +1 more source

PET imaging of M4 muscarinic acetylcholine receptors in rhesus macaques using [11C]MK-6884: Quantification with kinetic modeling and receptor occupancy by CVL-231 (emraclidine), a novel positive allosteric modulator

Journal of Cerebral Blood Flow and Metabolism
Stimulation of the M4 muscarinic acetylcholine receptor reduces striatal hyperdopaminergia, suggesting its potential as a therapeutic target for schizophrenia.
Vasily Belov, N. Guehl, Sridhar Duvvuri, Philip Iredale, Sung-Hyun Moon, M. Dhaynaut, Srinivas Chakilam, Alexander C. MacDonagh, Peter A Rice, Daniel L. Yokell, John J. Renger, G. El Fakhri, M. Normandin   +12 more
semanticscholar   +1 more source

The Prosperity and Adversity of M4 Muscarinic Acetylcholine Receptor Activators in the Treatment of Neuropsychiatric Disorders.

Journal of Medicinal Chemistry
Since the serendipitous discovery of chlorpromazine in the 1950s, almost all current anti-schizophrenia drugs utilize the same mode of action by blocking the dopamine receptors in the brain.
Boqun Liu, A. Christopoulos, D. Thal, B. Capuano, C. Valant, P. Scammells   +5 more
semanticscholar   +1 more source

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

In Vivo Modulation of Hippocampal Excitability by M4 Muscarinic Acetylcholine Receptor Activator: Implications for Treatment of Alzheimer's Disease and Schizophrenic Patients.

ACS Chemical Neuroscience, 2018
Abnormal hippocampal activity has been linked to impaired cognitive performance in Alzheimer's disease and schizophrenia, leading to a hypothesis that normalization of this activity may be therapeutically beneficial.
M. Popiolek, Y. Mandelblat-Cerf, D. Young, Jonathan Garst-Orozco, S. Lotarski, Eda Stark, Melissa Kramer, Christopher R Butler, R. Kozak   +8 more
semanticscholar   +1 more source

Structure-activity relationship of pyrazol-4-yl-pyridine derivatives for imaging the muscarinic acetylcholine receptor M4

Nuclear Medicine and Biology, 2022
Ahmed Haider, Xiaoyun Deng, Stefanie K. Pfister, Troels E Jeppesen, Xia Zhiwei, Jian Rong, T. Connors, T. Collier, L. Mu, R. Schibli, A. Christopoulos, C. Valant, Steven H. Liang   +12 more
semanticscholar   +1 more source

Synthesis and Characterization of Chiral 6-Azaspiro[2.5]Octanes as Potent and Selective Antagonists of the M4 Muscarinic Acetylcholine Receptor.

Bioorganic & Medicinal Chemistry Letters, 2021
Aaron M. Bender, Trever R. Carter, Matthew Spock, Alice L. Rodriguez, J. Dickerson, J. M. Rook, Sichen Chang, Aidong Qi, C. Presley, D. Engers, J. Harp, T. Bridges, C. Niswender, P. Conn, C. Lindsley   +14 more
semanticscholar   +1 more source

Systemic therapy for hormone receptor‐positive/human epidermal growth factor receptor 2‐negative early stage and metastatic breast cancer

Ca-A Cancer Journal for Clinicians, 2023
Laura A Huppert, Hope S Rugo
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