Results 1 to 10 of about 46,071 (240)

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

Is muscarinic receptor agonist effective and tolerant for schizophrenia? [PDF]

BMC Psychiatry
Background Several randomized clinical trials (RCTs) have recently examined the efficacy and tolerability of muscarinic receptor agonists in schizophrenia. However, whether therapeutics targeting muscarinic receptors improve symptom management and reduce
Xiaonan Guo, Rongshan Deng, Jianbo Lai, Shaohua Hu   +3 more
doaj   +2 more sources

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

Pharmacology Research & Perspectives
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.
Madeleine Merz, Charlotte Playle, Monika Palchaudhuri, Oliver Hucke, Ulrike Gross, Daniel Ursu   +5 more
doaj   +2 more sources

Antipsychotic-like effect of the muscarinic acetylcholine receptor agonist BuTAC in non-human primates. [PDF]

PLoS ONE, 2015
Cholinergic, muscarinic receptor agonists exhibit functional dopamine antagonism and muscarinic receptors have been suggested as possible future targets for the treatment of schizophrenia and drug abuse. The muscarinic ligand (5R,6R)-6-(3-butylthio-1,2,5-
Maibritt B Andersen, Carrie Hughes Croy, Ditte Dencker, Thomas Werge, Frank P Bymaster, Christian C Felder, Anders Fink-Jensen   +6 more
doaj   +1 more source

Oscillatory calcium release and sustained store-operated oscillatory calcium signaling prevents differentiation of human oligodendrocyte progenitor cells

Scientific Reports, 2022
Endogenous remyelination in demyelinating diseases such as multiple sclerosis is contingent upon the successful differentiation of oligodendrocyte progenitor cells (OPCs).
Richard A. Seidman, Heba Khattab, Jessie J. Polanco, Jacqueline E. Broome, Fraser J. Sim   +4 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

The Bronchoprotective Effects of Dual Pharmacology, Muscarinic Receptor Antagonist and β₂ Adrenergic Receptor Agonist Navafenterol in Human Small Airways

Cells, 2023
Bronchodilators and anti-inflammatory agents are the mainstream treatments in chronic obstructive and pulmonary disease (COPD) and asthma.
Joseph Antony Jude, Ian Dainty, Nikhil Karmacharya, William Jester, Reynold Panettieri   +4 more
doaj   +1 more source

A Cholinergic Synaptically Triggered Event Participates in the Generation of Persistent Activity Necessary for Eye Fixation [PDF]

, 2004
An exciting topic regarding integrative properties of the nervous system is how transient motor commands or brief sensory stimuli are able to evoke persistent neuronal changes, mainly as a sustained, tonic action potential firing.
Alvarado, JC, Delgado-Garcia, JM, Escudero, M, Marquez-Ruiz, J, Navarro-Lopez, J, Yajeya, J   +5 more
core   +5 more sources

The metronomic combination of paclitaxel with cholinergic agonists inhibits triple negative breast tumor progression. Participation of M2 receptor subtype

PLoS ONE, 2020
Triple negative tumors are more aggressive than other breast cancer subtypes and there is a lack of specific therapeutic targets on them. Since muscarinic receptors have been linked to tumor progression, we investigated the effect of metronomic therapy ...
Alejandro J. Español, Agustina Salem, María Di Bari, Ilaria Cristofaro, Yamila Sanchez, Ada M. Tata, María E. Sales, Irina V. Lebedeva   +7 more
doaj   +2 more sources

Functional characterization of three G protein-coupled acetylcholine receptors in parasitic nematode Trichinella spiralis

International Journal for Parasitology: Drugs and Drug Resistance, 2023
The physiological significance of metabotropic acetylcholine receptors in parasitic nematodes remains largely unexplored. Here, three different Trichinella spiralis G protein-coupled acetylcholine receptors (TsGAR-1, -2, and -3) were identified in the ...
Cáinà Nìng, Aurélie Heckmann, Lourdes Mateos-Hernández, Grégory Karadjian, Ladislav Šimo   +4 more
doaj   +1 more source