Results 31 to 40 of about 15,825 (259)

Dualsteric modulators of the M2 muscarinic acetylcholine receptor [PDF]

Journal of Cheminformatics, 2014
G-protein coupled receptors (GPCRs) trigger multiple signal-switching mechanisms like binding of s-arrestin proteins, activation of kinases and G-protein activation [1]. The poor understanding of the conformational changes resulting in these activations is a major challenge for the design of specific GPCR modulating drugs.
Gerhard Wolber, Marcel Bermudez
openaire   +2 more sources

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

Internalization of the m2 Muscarinic Acetylcholine Receptor [PDF]

Journal of Biological Chemistry, 1997
Recent studies have identified agonist-dependent phosphorylation as a critical event in the rapid uncoupling of the m2 muscarinic cholinergic receptors (mAChR) from G-proteins and sequestration of the receptors away from the cell surface. However, mutant m2 mAChRs were identified that were phosphorylated but unable to desensitize in adenylyl cyclase ...
Katharine B. Lee, Robin Pals-Rylaarsdam, M. Marlene Hosey, Vsevolod V. Gurevich, Judith A. Ptasienski, Jeffrey L. Benovic   +5 more
openaire   +3 more sources

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

On homology modeling of the M2 muscarinic acetylcholine receptor subtype [PDF]

Journal of Computer-Aided Molecular Design, 2013
Twelve homology models of the human M(2) muscarinic receptor using different sets of templates have been designed using the Prime program or the modeller program and compared to crystallographic structure (PDB:3UON). The best models were obtained using single template of the closest published structure, the M(3) muscarinic receptor (PDB:4DAJ).
Jan Jakubík, Alena Randáková, Vladimír Doležal   +2 more
openaire   +2 more sources

Porcine m2 Muscarinic Acetylcholine Receptor-Effector Coupling in Chinese Hamster Ovary Cells [PDF]

Journal of Biological Chemistry, 1995
The relationship between porcine m2 muscarinic receptor coupling to inhibition of cAMP formation and stimulation of phosphatidylinositol metabolism in Chinese hamster ovary cells was examined. Reduction of the number of receptors per cell with the slowly dissociating antagonist (-)-quinuclidinyl benzilate caused a decrease in maximal response with no ...
W. Vogel, Valerie A. Mosser, Dylan A. Bulseco, Michael I. Schimerlik   +3 more
openalex   +5 more sources

Unraveling a molecular determinant for clathrin-independent internalization of the M2 muscarinic acetylcholine receptor [PDF]

Scientific Reports, 2015
AbstractEndocytosis and postendocytic sorting of G-protein-coupled receptors (GPCRs) is important for the regulation of both their cell surface density and signaling profile. Unlike the mechanisms of clathrin-dependent endocytosis (CDE), the mechanisms underlying the control of GPCR signaling by clathrin-independent endocytosis (CIE) remain largely ...
Min Wan, Wenhua Zhang, Yangli Tian, Chanjuan Xu, Tao Xu, Jianfeng Liu, Rongying Zhang   +6 more
openalex   +4 more sources

Dysfunctional Presynaptic M2 Receptors in the Presence of Chronically High Acetylcholine Levels: Data from the PRiMA Knockout Mouse. [PDF]

PLoS ONE, 2015
The muscarinic M2 receptor (M2R) acts as a negative feedback regulator in central cholinergic systems. Activation of the M2 receptor limits acetylcholine (ACh) release, especially when ACh levels are increased because acetylcholinesterase (AChE) activity
Franziska Mohr, Eric Krejci, Martina Zimmermann, Jochen Klein   +3 more
doaj   +1 more source

Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers [PDF]

, 2015
Each subtype of the muscarinic receptor family of G protein-coupled receptors is activated by similar concentrations of the neurotransmitter acetylcholine or closely related synthetic analogs such as carbachol. However, pharmacological selectivity can be
Alvarez-Curto, Elisa, Aslanoglou, Despoina, Marsango, Sara, Milligan, Graeme   +3 more
core   +1 more source