Results 11 to 20 of about 6,629 (211)

Exploring Adjunctive Novel Therapeutic Approach of KarXT (Xanomeline-Trospium Chloride) for Managing Psychotic Symptoms in Patients With Schizophrenia and Alzheimer's Disease. [PDF]

Brain Behav
An overview of the mechanism of action, clinical trials, and classical findings of KarXT for the management of psychotic symptoms in patients with schizophrenia and alzheimer's disease. ABSTRACT Background Acute psychotic symptoms like delusions and hallucinations are of major concern while treating patients with schizophrenia and alzheimer's psychosis,
Kanwal A, Azeem B, Nasir H, Mumtaz F, Ashraf N, Amin MHJ, Kanwal W, Khan BW.   +7 more
europepmc   +2 more sources

Downstream Signaling of Muscarinic M₄ Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]

Pharmacol Res Perspect
ABSTRACT Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators. Considering the importance of comprehending M4 receptor pharmacology for these therapeutic applications, this study investigates M4 receptor ...
Merz M, Playle C, Palchaudhuri M, Hucke O, Gross U, Ursu D.   +5 more
europepmc   +2 more sources

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of ¹⁸F-Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3. [PDF]

ChemMedChem
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Herrera-Rueda MA, Boateng MA, Wuest M, West FG, Wuest F.   +4 more
europepmc   +2 more sources

Rationale for Selective Muscarinic Receptor Agonists as Candidates for the Management of Cognitive and Neuropsychiatric Symptoms in Alzheimer's Disease [PDF]

Alzheimers Dement
Abstract Background Cognitive impairment and neuropsychiatric symptoms, including psychosis, are fundamental features of Alzheimer's disease (AD) and related dementias. Currently treatments for these symptoms have efficacy, safety, and tolerability limitations; new treatments with novel mechanisms are needed.
Marcus R, Vuocolo S, Ramsey I, Watson C, Kang M.   +4 more
europepmc   +2 more sources

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors [PDF]

Nature, 2016
Muscarinic M1-M5 acetylcholine receptors are G-protein-coupled receptors that regulate many vital functions of the central and peripheral nervous systems. In particular, the M1 and M4 receptor subtypes have emerged as attractive drug targets for treatments of neurological disorders, such as Alzheimer's disease and schizophrenia, but the high ...
David M, Thal, Bingfa, Sun, Dan, Feng, Vindhya, Nawaratne, Katie, Leach, Christian C, Felder, Mark G, Bures, David A, Evans, William I, Weis, Priti, Bachhawat, Tong Sun, Kobilka, Patrick M, Sexton, Brian K, Kobilka, Arthur, Christopoulos   +13 more
openaire   +2 more sources

Xanomeline displays concomitant orthosteric and allosteric binding modes at the M4 mAChR

Nature Communications, 2023
The M4 muscarinic acetylcholine receptor (M4 mAChR) has emerged as a drug target of high therapeutic interest due to its expression in regions of the brain involved in the regulation of psychosis, cognition, and addiction.
Wessel A. C. Burger, Vi Pham, Ziva Vuckovic, Alexander S. Powers, Jesse I. Mobbs, Yianni Laloudakis, Alisa Glukhova, Denise Wootten, Andrew B. Tobin, Patrick M. Sexton, Steven M. Paul, Christian C. Felder, Radostin Danev, Ron O. Dror, Arthur Christopoulos, Celine Valant, David M. Thal   +16 more
doaj   +1 more source

The structural study of mutation-induced inactivation of human muscarinic receptor M4

IUCrJ, 2020
Human muscarinic receptor M4 belongs to the class A subfamily of the G-protein-coupled receptors (GPCRs). M4 has emerged as an attractive drug target for the treatment of Alzheimer's disease and schizophrenia.
Jingjing Wang, Meng Wu, Lijie Wu, Yueming Xu, Fei Li, Yiran Wu, Petr Popov, Lin Wang, Fang Bai, Suwen Zhao, Zhi-Jie Liu, Tian Hua   +11 more
doaj   +1 more source

Increased cocaine self-administration in M4 muscarinic acetylcholine receptor knockout mice [PDF]

Psychopharmacology, 2011
The reinforcing effects of cocaine are mediated by the mesolimbic dopamine system. Behavioral and neurochemical studies have shown that the cholinergic muscarinic M(4) receptor subtype plays an important role in regulation of dopaminergic neurotransmission.Here we investigated for the first time the involvement of M(4) receptors in the reinforcing ...
Schmidt, Lene Sørensen, Thomsen, Morgane, Weikop, Pia, Nielsen, Ditte Dencker, Wess, Jürgen, Woldbye, David Paul Drucker, Wörtwein, Gitta, Fink-Jensen, Anders   +7 more
openaire   +3 more sources

Live-cell microscopy or fluorescence anisotropy with budded baculoviruses—which way to go with measuring ligand binding to M4 muscarinic receptors?

Open Biology, 2022
M4 muscarinic acetylcholine receptor is a G protein-coupled receptor (GPCR) that has been associated with alcohol and cocaine abuse, Alzheimer's disease, and schizophrenia which makes it an interesting drug target.
Maris-Johanna Tahk, Jane Torp, Mohammed A. S. Ali, Dmytro Fishman, Leopold Parts, Lukas Grätz, Christoph Müller, Max Keller, Santa Veiksina, Tõnis Laasfeld, Ago Rinken   +10 more
doaj   +1 more source

Novel Interaction between the M4 Muscarinic Acetylcholine Receptor and Elongation Factor 1A2 [PDF]

Journal of Biological Chemistry, 2002
The activation of the muscarinic acetylcholine receptor (mAChR) family, consisting of five subtypes (M1-M5), produces a variety of physiological effects throughout the central nervous system. However, the role of each individual subtype remains poorly understood.
McClatchy, D.B., Knudsen, C.R., Clark, Brian F. C., Kahn, R.A., Hall, R.A., Levey, A.I.   +5 more
openaire   +3 more sources