Results 71 to 80 of about 40,413 (202)

Muscarinic agonists for schizophrenia: Bridging preclinical evidence and clinical enthusiasm

British Journal of Pharmacology, Volume 183, Issue 19, Page 5701-5731, October 2026.
Abstract Antipsychotic drugs targeting dopamine receptors have been used to treat schizophrenia for decades, primarily alleviating positive symptoms such as hallucinations and delusions. However, they provide limited benefit for cognitive and negative symptoms—major contributors to poor outcomes—and are frequently associated with significant side ...
Brian J. Morris, Judith A. Pratt
wiley   +1 more source

Advances in Targeting Central Cholinergic Dysfunction for Neurodegenerative Diseases: From Pharmacotherapy to Neuromodulation

CNS Neuroscience &Therapeutics, Volume 32, Issue 9, September 2026.
This review charts the evolution of cholinergic therapies for neurodegenerative diseases—from classical acetylcholinesterase inhibitors (AChEIs) providing symptomatic relief to precision multi‐target drugs and neuromodulation (VNS, DBS, NIBS) that restore dysfunctional circuits. Emerging gene therapy, cell regeneration, and advanced cholinergic imaging
Lei Lei, Xiaoyu Hu, Ruida Lu, Jian‐jun Yang, Qingsheng Meng   +4 more
wiley   +1 more source

Design, Synthesis, and Evaluation of a New Fluorescent Ligand for the M2 Muscarinic Acetylcholine Receptor

ACS Medicinal Chemistry Letters
The M2 muscarinic acetylcholine receptor (M2R) is a G protein-coupled receptor involved in regulating cardiovascular functions and mediation of central muscarinic effects, such as movement, temperature control, and antinociceptive responses.
Renáta Szabó, Dénes Szepesi Kovács, D. J. Kiss, Z. Yazdi, A. Tóth, J. Brea, M. Loza, Domokos Meszéna, Lucia Wittner, I. Ulbert, Balázs Volk, László Hunyady, G. Keserű   +12 more
semanticscholar   +1 more source

M5 Muscarinic Receptor Gene Deletion Accelerates Extinction, But Inhibits Reinstatement of Morphine-Conditioned Reward in Mice

, 2017
Mesolimbic dopamine neurons in the ventral tegmental area (VTA) play important roles in mediating the rewarding effects of opiates in addicted rats and in drug relapse.
Haoran G. Wang
semanticscholar   +1 more source

Hypothalamic Control of Liver Health and Disease: From Circuits to Pathophysiology and Therapies

Advanced Science, Volume 13, Issue 47, 24 August 2026.
This review delineates the hypothalamic circuits that control liver homeostasis via autonomic and neuroendocrine pathways. Dysregulation of this hypothalamus–liver axis drives disease progression across a spectrum including steatotic liver disease, liver inflammation and injury, fibrosis, cirrhosis, and hepatocellular carcinoma.
Qin Tang, Jiahui Li, Haiying Song, Ailin Zhang, Haifeng Zeng, Yining Xu, Li Mo, Jinhan He   +7 more
wiley   +1 more source

Redirecting Alzheimer's disease therapeutics: Multitarget drugs and complementary non‐pharmacological strategies

Alzheimer's &Dementia, Volume 22, Issue 6, June 2026.
Abstract Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder driven by intersecting pathological processes. Persistent attrition in AD drug‐development pipelines highlights the limited clinical impact of single‐target therapies and has increased interest in multi‐target approaches acting on shared biological hubs.
Humberto Martínez‐Orozco, Jesús Andrade‐Guerrero, Nelly Jovana Pastén‐Castrejón, Chryslaine Rodríguez‐Tanty, Sofía Y Diaz‐Miranda   +4 more
wiley   +1 more source

Repositioning VU‐0365114 as a novel microtubule‐destabilizing agent for treating cancer and overcoming drug resistance

Molecular Oncology
Microtubule‐targeting agents represent one of the most successful classes of anticancer agents. However, the development of drug resistance and the appearance of adverse effects hamper their clinical implementation.
Yao‐Yu Hsieh, Jia‐Ling Du, Pei‐Ming Yang   +2 more
doaj   +1 more source

Regulation of Src family kinases by muscarinic acetylcholine receptors in heterologous cells and neurons

Frontiers in Molecular Neuroscience
Five muscarinic acetylcholine (mACh) receptor subtypes are divided into two classes: the M1 class (M1, M3, and M5) and the M2 class (M2 and M4). The former is coupled to Gq proteins, while the latter is coupled to Gi/o proteins.
Li-Min Mao, Lexi Young, Xiang-Ping Chu, John Q. Wang, John Q. Wang   +4 more
doaj   +1 more source

Ligand bias at the muscarinic acetylcholine receptor family: opportunities and challenges.

Neuropharmacology
Muscarinic acetylcholine receptors (mAChRs) are G protein-coupled receptors (GPCRs) that are activated by the endogenous neurotransmitter, acetylcholine (ACh).
Michaela G. Kaoullas, D. Thal, A. Christopoulos, C. Valant   +3 more
semanticscholar   +1 more source

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)

Journal of Medicinal Chemistry, 2013
A functional high throughput screen and subsequent multi-dimensional, iterative parallel synthesis effort identified the first muscarinic acetylcholine receptor (mAChR) negative allosteric modulator (NAM) selective for the M5 subtype.
P. R. Gentry, M. Kokubo, T. M. Bridges, Nathan R Kett, J. Harp, Hyekyung P. Cho, Emery Smith, P. Chase, P. Hodder, C. Niswender, J. S. Daniels, P. Conn, M. Wood, C. Lindsley   +13 more
semanticscholar   +1 more source