Results 1 to 10 of about 16,354 (156)

Structural determinants at the M2 muscarinic receptor modulate the RGS4-GIRK response to pilocarpine by impairment of the receptor voltage sensitivity [PDF]

Scientific Reports, 2017
Membrane potential controls the response of the M2 muscarinic receptor to its ligands. Membrane hyperpolarization increases response to the full agonist acetylcholine (ACh) while decreasing response to the partial agonist pilocarpine.
I-Shan Chen, Kazuharu Furutani, Yoshihisa Kurachi   +2 more
doaj   +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

Recovery of hippocampal functions and modulation of muscarinic response by electroacupuncture in young diabetic rats [PDF]

Scientific Reports, 2017
The muscarinic receptor response to acetylcholine regulates the hippocampal-related learning, memory, neural plasticity and the production and processing of the pro-nerve growth factor (proNGF) by hippocampal cells.
Marzia Soligo, Sonia Piccinin, Virginia Protto, Francesca Gelfo, Maria Egle De Stefano, Fulvio Florenzano, Erica Berretta, Laura Petrosini, Robert Nisticò, Luigi Manni   +9 more
doaj   +3 more sources

Pathogenic Gαo Mutants Drive Dominant GPCR Coupling in GNAO1 Encephalopathies. [PDF]

FASEB J
Mutations in GNAO1, the gene encoding Gαo, are associated with a wide range of neurodevelopmental disorders. In this study, we show that Gαo variants linked to the most severe patient phenotypes fail to disengage from activated Gi/o‐coupled GPCRs, thereby blocking GRK‐mediated receptor phosphorylation and internalization.
Larasati YA, de Meritens CR, Stoeber M, Katanaev VL, Solis GP.   +4 more
europepmc   +2 more sources

Changes in adrenergic and cholinergic receptors on human cerebral vessels. Implications for new therapeutic strategies in Alzheimer's Disease [PDF]

Alzheimers Dement
Abstract Background Sporadic cerebral amyloid angiopathy (CAA) occurs as a result of a failure of Intramural Periarterial Drainage (IPAD) of amyloid‐beta (Aβ) along the walls of capillaries and arteries. The motive force for IPAD is provided by the spontaneous contractions of cerebrovascular smooth muscle cells (CVSMC that receive adrenergic and ...
Carare R.
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

Further Insights Into Anticholinergic Action Informed by Japanese Anticholinergic Risk Scale. [PDF]

Geriatr Gerontol Int
ABSTRACT The increased anticholinergic burden caused by medications in older adults is one of the adverse drug reactions of particular concern, as it can exacerbate the onset of geriatric syndromes or induce cognitive dysfunction, and is also related to the issue of polypharmacy.
Mogi M, Liu S, Suzuki Y, Shibata Y, Yamada S.   +4 more
europepmc   +2 more sources

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

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

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