Results 251 to 260 of about 30,424 (296)
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Constitutive Activity and Inverse Agonism at the M2 Muscarinic Acetylcholine Receptor
The Journal of Pharmacology and Experimental Therapeutics, 2006Introduction of a single-point mutation (Asn to Tyr) at position 410 at the junction between transmembrane domain 6 and the third extracellular loop of the human M(2) muscarinic acetylcholine (mACh) receptor generated a mutant receptor (N410Y) that possesses many of the hallmark features of a constitutively active mutant receptor.
Nelson, Carl P. +2 more
openaire +3 more sources
, 2018
Human muscarinic receptor M2 is one of the five subtypes of muscarinic receptors belonging to the family of G-protein-coupled receptors. Muscarinic receptors are targets for multiple neurodegenerative diseases.
Ryoji Suno +15 more
semanticscholar +1 more source
Human muscarinic receptor M2 is one of the five subtypes of muscarinic receptors belonging to the family of G-protein-coupled receptors. Muscarinic receptors are targets for multiple neurodegenerative diseases.
Ryoji Suno +15 more
semanticscholar +1 more source
Structure-Function Studies of Allosteric Agonism at M2 Muscarinic Acetylcholine Receptors
Molecular Pharmacology, 2007The M2 muscarinic acetylcholine receptor (mAChR) possesses at least one binding site for allosteric modulators that is dependent on the residues (172)EDGE(175), Tyr(177), and Thr(423). However, the contribution of these residues to actions of allosteric agonists, as opposed to modulators, is unknown.
Lauren T, May +6 more
openaire +2 more sources
Nature of the oligomers formed by muscarinic m2 acetylcholine receptors in Sf9 cells
European Journal of Pharmacology, 2001Wild-type, FLAG-tagged, and c-myc-tagged muscarinic m2 receptors extracted in digitonin-cholate from singly and co-infected Sf9 (Spodoptera frugiperda) cells were indistinguishable in their binding of [3H]quinuclidinylbenzilate, either before or after purification.
P, Park +4 more
openaire +2 more sources
Interaction of Edrophonium with Muscarinic Acetylcholine M2and M3Receptors
Anesthesiology, 2001Background It has been reported that edrophonium can antagonize the negative chronotropic effect of carbachol. This study was undertaken to evaluate in detail the interaction of edrophonium with muscarinic Mz and M3 receptors. Methods A functional study was conducted to evaluate the
Y, Tanito +6 more
openaire +2 more sources
European Journal of Neuroscience, 2020
Acetylcholine (ACh) modulates neurotransmitter release in the central nervous system. Although GABAergic transmission onto the striatal cholinergic interneurons (ChIN) is modulated by dopamine receptors, cholinergic modulation of the same synapse is ...
Etsuko Suzuki, T. Momiyama
semanticscholar +1 more source
Acetylcholine (ACh) modulates neurotransmitter release in the central nervous system. Although GABAergic transmission onto the striatal cholinergic interneurons (ChIN) is modulated by dopamine receptors, cholinergic modulation of the same synapse is ...
Etsuko Suzuki, T. Momiyama
semanticscholar +1 more source
Molecular Pharmacology, 1998
Muscarinic acetylcholine receptors bind allosteric modulators at a site apart from the orthosteric site used by conventional ligands. We tested in cardiac tissue whether modulator binding to ligand-occupied muscarinic M2 receptors is a preferential event that can be detected using a radioactive allosteric agent. The newly synthesized dimethyl-W84 (N,N'-
C, Tränkle +4 more
openaire +2 more sources
Muscarinic acetylcholine receptors bind allosteric modulators at a site apart from the orthosteric site used by conventional ligands. We tested in cardiac tissue whether modulator binding to ligand-occupied muscarinic M2 receptors is a preferential event that can be detected using a radioactive allosteric agent. The newly synthesized dimethyl-W84 (N,N'-
C, Tränkle +4 more
openaire +2 more sources
Biochemical and Biophysical Research Communications, 1988
Neuraminidase and slight acid hydrolysis were used to investigate the role of sialic acid residues in the binding of muscarinic agonists and antagonists to membranes from tissues rich in M1 and M2 receptors. Membranes were pretreated with neuraminidase at pH 5 and the binding parameters were determined from competitive experiments with (3H ...
J P, Gies, Y, Landry
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Neuraminidase and slight acid hydrolysis were used to investigate the role of sialic acid residues in the binding of muscarinic agonists and antagonists to membranes from tissues rich in M1 and M2 receptors. Membranes were pretreated with neuraminidase at pH 5 and the binding parameters were determined from competitive experiments with (3H ...
J P, Gies, Y, Landry
openaire +2 more sources
The M2 muscarinic receptor, in association to M1, regulates the neuromuscular PKA molecular dynamics
The FASEB Journal, 2020Muscarinic acetylcholine receptor 1 subtype (M1) and muscarinic acetylcholine receptor 2 subtype (M2) presynaptic muscarinic receptor subtypes increase and decrease, respectively, neurotransmitter release at neuromuscular junctions.
V. Cilleros-Mañé +5 more
semanticscholar +1 more source
Effects of Autoantibodies against M2 Muscarinic Acetylcholine Receptors on Rabbit Atria in vivo
Cardiology, 2008<i>Background:</i> Evidence has shown that autoantibodies against M2 muscarinic acetylcholine receptors may play a role in the development of atrial fibrillation. The goal of this study was to evaluate the effects of anti-M2 receptor autoantibodies on rabbit atria in vivo.
Chang Ming, Hong +5 more
openaire +2 more sources