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 +8 more
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Pronounced pharmacologic deficits in M2 muscarinic acetylcholine receptor knockout mice [PDF]
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 +8 more
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Expression of Functional M2 Muscarinic Acetylcholine Receptor in Escherichia coli [PDF]
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
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Modulation of the M2 Muscarinic Acetylcholine Receptor Activity with Monoclonal Anti-M2 Receptor Antibody Fragments [PDF]
Antibodies directed against the second extracellular loop of G protein-coupled receptors are known to have functional activities. From a partial agonist monoclonal antibody directed against the M2 muscarinic receptor, we constructed and produced a single chain variable fragment with high affinity for its target epitope.
Jean-Christophe, Peter +6 more
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Synergistic regulation mechanism of iperoxo and LY2119620 for muscarinic acetylcholine M2 receptor [PDF]
Dynamics correlation network was used to reveal the synergistic regulation mechanism of iperoxo and LY2119620 for muscarinic acetylcholine M2 receptor.
Quan Li, Hai-Feng Chen
openaire +4 more sources
.: Intestinal myofibroblasts (IMFs) that exist adjacent to the basement membrane of intestines have contractility and contribute to physical barriers of the intestine.
Koichi Iwanaga +4 more
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Dysfunctional Presynaptic M2 Receptors in the Presence of Chronically High Acetylcholine Levels: Data from the PRiMA Knockout Mouse. [PDF]
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 +3 more
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Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype
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 +5 more
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Pathogenic Gαo Mutants Drive Dominant GPCR Coupling in GNAO1 Encephalopathies. [PDF]
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 +4 more
europepmc +2 more sources
Position of anticholinergic drugs in the treatment of childhood asthma [PDF]
Anticholinergic drugs block muscarinic effect of acetylcholine on the receptors of postjunctional membranes and so inhibit the answer of the postganglionic parasympathetic nerve.
Stojković-Anđelković Anđelka +3 more
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