Results 31 to 40 of about 30,424 (296)

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.
Bermudez, Marcel, Wolber, Gerhard
openaire   +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

Expression of Functional M2 Muscarinic Acetylcholine Receptor in Escherichia coli [PDF]

Journal of Biochemistry, 2000
The M2 muscarinic acetylcholine receptor mutant (M2 mutant), with a lack of glycosylation sites, a deletion in the central part of the third inner loop, and the addition of a six histidine tag at the C-terminus, was fused to maltose binding protein (MBP) at its N-terminus and expressed in Escherichia coli. The expression level was 0.2 nmol receptor per
H, Furukawa, T, Haga
openaire   +2 more sources

Characterization of the positive and negative inotropic effects of acetylcholine in the human myocardium [PDF]

, 1995
In the human isolated myocardium, acetylcholine (10−9 to 10−3 M) elicited a biphasic inotropic effect (a decrease in the lower and an increase in the higher concentration range) in atrial and a positive inotropic effect in ventricular trabeculae. However,
Bos, E. (Egbert), Du, X.Y. (Xiaoyi), Saxena, P.R. (Pramod Ranjan), Schoemaker, R.G. (Regien)   +3 more
core   +7 more sources

Agonist-Specific Conformations of the M2 Muscarinic Acetylcholine Receptor Assessed by Molecular Dynamics

Journal of Chemical Information and Modeling, 2020
Binding of muscarinic ligands, both antagonists and agonists, and their effects on the conformation of the M2 acetylcholine receptor were modeled in silico and compared to experimental data.
Alena Randáková, Dominik Nelic, V. Doležal, E. E. El-Fakahany, John Boulos, J. Jakubík   +5 more
semanticscholar   +1 more source

Pronounced pharmacologic deficits in M2 muscarinic acetylcholine receptor knockout mice. [PDF]

Proceedings of the National Academy of Sciences, 1999
Members of the muscarinic acetylcholine receptor family (M1–M5) are known to be involved in a great number of important central and peripheral physiological and pathophysiological processes. Because of the overlapping expression patterns of the M1–M5 muscarinic receptor subtypes and the lack of ligands endowed with sufficient subtype selectivity ...
J. Gomeza, H. Shannon, E. Kostenis, C. Felder, Lu Zhang, J. Brodkin, A. Grinberg, Hui Sheng, J. Wess   +8 more
semanticscholar   +3 more sources

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

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

Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

Journal of Pharmacological Sciences, 2004
Heterologous down-regulation of histamine H1 receptor (H1R) mediated by muscarinic acetylcholine receptor subtype was investigated using five kinds of Chinese hamster ovary (CHO) cells stably co-expressing the human H1R and one of the five (M1 –M5 ...
Katsuhiro Miyoshi, Nozomi Kawakami, Yousuke Wakayama, Norimasa Izumi, Shuhei Horio, Hiroyuki Fukui   +5 more
doaj   +1 more source