Results 11 to 20 of about 12,342 (188)

Revisiting the Endocytosis of the M2 Muscarinic Acetylcholine Receptor [PDF]

open access: yesMembranes, 2015
The agonist-induced endocytosis of the muscarinic acetylcholine receptor M2 is different from that of the other members of the muscarinic receptor family.
Wymke Ockenga, Ritva Tikkanen
doaj   +3 more sources

Voltage affects the dissociation rate constant of the m2 muscarinic receptor. [PDF]

open access: yesPLoS ONE, 2013
G-protein coupled receptors (GPCRs) comprise the largest protein family and mediate the vast majority of signal transduction processes in the body. Until recently GPCRs were not considered to be voltage dependent.
Yair Ben Chaim   +3 more
doaj   +5 more sources

Activation and dynamic network of the M2 muscarinic receptor [PDF]

open access: yesProceedings of the National Academy of Sciences, 2013
G-protein-coupled receptors (GPCRs) mediate cellular responses to various hormones and neurotransmitters and are important targets for treating a wide spectrum of diseases. Although significant advances have been made in structural studies of GPCRs, details of their activation mechanism remain unclear.
Yinglong, Miao   +4 more
openaire   +2 more sources

Dualsteric modulators of the M2 muscarinic acetylcholine receptor [PDF]

open access: yesJournal 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.
Marcel Bermudez, Gerhard Wolber
openaire   +1 more source

Sodium ions allosterically modulate the M2 muscarinic receptor [PDF]

open access: yesScientific Reports, 2020
AbstractG protein coupled receptors (GPCRs) play a key role in the vast majority of cellular signal transduction processes. Previous experimental evidence has shown that sodium ion (Na+) allosterically modulate several class A GPCRs and theoretical studies suggested that the same also holds true for muscarinic receptors. Here we examined, using Xenopus
Friedman, Sheli   +2 more
openaire   +2 more sources

Effects of tetrahydroaminoacridine on M1 and M2 muscarine receptors

open access: yesNeuroscience Letters, 1988
Tetrahydroaminoacridine (THA) has been reported to improve the memory of persons with Alzheimer's disease, but its mechanism of action is uncertain. We found that clinically effective concentrations, 0.03-0.3 microM, readily inhibit acetylcholinesterase and butyrylcholinesterase from rabbit hippocampal tissue in artificial cerebrospinal fluid (CSF) at ...
B D, Pearce, L T, Potter
openaire   +2 more sources

Regulation of signal transduction at M2 muscarinic receptor

open access: yesPhysiological Research, 2004
Muscarinic acetylcholine receptors mediate transmission of an extracellular signal represented by released acetylcholine to neuronal or effector cells. There are five subtypes of closely homologous muscarinic receptors which are coupled by means of heterotrimeric G-proteins to a variety of signaling pathways resulting in a multitude of target cell ...
A, Krejcí   +4 more
openaire   +2 more sources

Evidence for M2 and M3 Muscarinic Receptor Involvement in Cholinergic Excitatory Junction Potentials Through Synergistic Activation of Cation Channels in the Longitudinal Muscle of Mouse Ileum

open access: yesJournal of Pharmacological Sciences, 2013
Cholinergic nerve–mediated excitatory junction potentials (EJPs) in the longitudinal muscle of mouse ileum were characterized by using M2 or M3 muscarinic receptor–knockout (KO) mice and 1-[β-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole ...
Hayato Matsuyama   +5 more
doaj   +1 more source

Muscarinic receptor regulation of chronic pain-induced atrial fibrillation

open access: yesFrontiers in Cardiovascular Medicine, 2022
Atrial fibrillation (AF), one of the most common arrhythmias, is associated with chronic emotional disorder. Chronic pain represents a psychological instability condition related to cardiovascular diseases, but the mechanistic linkage connecting chronic ...
Chao Gong   +10 more
doaj   +1 more source

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

open access: yesPLoS 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   +3 more
doaj   +1 more source

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