Results 1 to 10 of about 8,482 (134)

Xanomeline and Trospium Chloride: Mechanism of Action, Clinical, and Translational Science. [PDF]

Clin Transl Sci
ABSTRACT Xanomeline‐trospium chloride (Cobenfy, formerly KarXT) is a first‐in‐class, oral central M1/M4 muscarinic receptor agonist approved for the treatment of schizophrenia in adults. Cobenfy represents a paradigm shift by avoiding direct dopamine D2 receptor blockade and thus significantly reduces the burden of metabolic, extrapyramidal, and ...
Avila S, Chen IL.
europepmc   +2 more sources

The dual-site agonist for human M2 muscarinic receptors Iper-8-naphtalimide induces mitochondrial dysfunction in Saccharomyces cerevisiae [PDF]

Microbial Cell
Glioblastoma is a malignant astrocytic tumor of the brain. A significantly decrease of glioblastoma cell proliferation and survival can be achieved by activating the M2 muscarinic acetylcholine receptor (a G protein-coupled receptor, or GPCR) with two ...
Angela Cirigliano, Antonia Amelina, Elena Passarini, Alessandra Ricelli, Nicole Balasco, Mattia Mori, Bruno Botta, Maria Egle De Stefano, Claudio Papotto, Claudia Guerriero, Ada Maria Tata, Teresa Rinaldi   +11 more
doaj   +2 more sources

Advances in Targeting Central Cholinergic Dysfunction for Neurodegenerative Diseases: From Pharmacotherapy to Neuromodulation. [PDF]

CNS Neurosci Ther
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 L, Hu X, Lu R, Yang JJ, Meng Q.
europepmc   +2 more sources

Hypothalamic Control of Liver Health and Disease: From Circuits to Pathophysiology and Therapies. [PDF]

Adv Sci (Weinh)
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.
Tang Q, Li J, Song H, Zhang A, Zeng H, Xu Y, Mo L, He J.   +7 more
europepmc   +2 more sources

Synergistic mechanisms of medullary cholinergic-serotonergic pathway interactions in regulating neuronal excitability and locomotor activities [PDF]

Communications Biology
Medullary serotonergic (5-HT) neurons play a pivotal role in locomotor initiation. While these neurons receive cholinergic innervation, the functional consequences and underlying mechanisms remain poorly understood. Using ePet-EYFP transgenic mice (P3–P6)
Yi Cheng, Yue Dai, Renkai Ge, Qiang Zhang   +3 more
doaj   +2 more sources

Muscarinic receptor regulation of chronic pain-induced atrial fibrillation

Frontiers in Cardiovascular Medicine, 2022
Atrial fibrillation (AF), one of the most common arrhythmias, is associated with chronic emotional disorder. Chronic pain represents a psychological instability condition related to cardiovascular diseases, but the mechanistic linkage connecting chronic ...
Chao Gong, Yu Ding, Feng Liang, Shuang Wu, Xiruo Tang, Hongzhang Ding, Wenjing Huang, Xiaotong Yu, Likun Zhou, Jun Li, Shaowen Liu   +10 more
doaj   +1 more source

Involvement of muscarinic receptors in psychomotor hyperactivity in dopamine-deficient mice

Molecular Brain, 2022
Dopamine-deficient (DD) mice exhibit psychomotor hyperactivity that might be related to a decrease in muscarinic signaling. In the present study, muscarinic acetylcholine receptor M2 (CHRM2) density decreased in the cortex in DD mice. This is significant
Masayo Fujita, Yukiko Ochiai, Yoko Hagino, Kazuto Kobayashi, Geoffrey Pavey, Brian Dean, Kazutaka Ikeda   +6 more
doaj   +1 more source

General anaesthesia-related complications of gut motility with a focus on cholinergic mechanisms, TRP channels and visceral pain

Frontiers in Physiology, 2023
General anesthesia produces multiple side effects. Notably, it temporarily impairs gastrointestinal motility following surgery and causes the so-called postoperative ileus (POI), a multifactorial and complex condition that develops secondary to ...
Alexander V. Zholos, Dariia O. Dryn, Mariia I. Melnyk, Mariia I. Melnyk   +3 more
doaj   +1 more source

Vibrational spectroscopy analysis of ligand efficacy in human M2 muscarinic acetylcholine receptor (M2R)

Communications Biology, 2021
Katayama et al. report a vibrational spectroscopic study using ATR–FTIR of the human M2 muscarinic acetylcholine receptor (M2R). Their work involves an extensive comparison of agonists, antagonists, and inverse agonists, in which they show that they C ...
Kota Katayama, Kohei Suzuki, Ryoji Suno, Ryoji Kise, Hirokazu Tsujimoto, So Iwata, Asuka Inoue, Takuya Kobayashi, Hideki Kandori   +8 more
doaj   +1 more source

Carbachol Induces Ca2+-Dependent Contraction via Muscarinic M2 and M3 Receptors in Rat Intestinal Subepithelial Myofibroblasts

Journal of Pharmacological Sciences, 2009
.: Intestinal myofibroblasts (IMFs) that exist adjacent to the basement membrane of intestines have contractility and contribute to physical barriers of the intestine.
Koichi Iwanaga, Takahisa Murata, Muneyoshi Okada, Masatoshi Hori, Hiroshi Ozaki   +4 more
doaj   +1 more source