Structural determinants at the M2 muscarinic receptor modulate the RGS4-GIRK response to pilocarpine by impairment of the receptor voltage sensitivity [PDF]
Scientific Reports, 2017 Membrane potential controls the response of the M2 muscarinic receptor to its ligands. Membrane hyperpolarization increases response to the full agonist acetylcholine (ACh) while decreasing response to the partial agonist pilocarpine.
I-Shan Chen +2 more
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Is muscarinic receptor agonist effective and tolerant for schizophrenia? [PDF]
BMC PsychiatryBackground Several randomized clinical trials (RCTs) have recently examined the efficacy and tolerability of muscarinic receptor agonists in schizophrenia. However, whether therapeutics targeting muscarinic receptors improve symptom management and reduce
Xiaonan Guo +3 more
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Muscarinic receptor oligomerization [PDF]
Neuropharmacology, 2018 G protein-coupled receptors (GPCRs) have been classically described as monomeric entities that function by binding in a 1:1 stoichiometric ratio to both ligand and downstream signalling proteins.
Alvarez-Curto, Elisa +3 more
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Characterization of Bladder Selectivity of Antimuscarinic Agents on the Basis of Drug-Receptor Binding [PDF]
International Neurourology Journal, 2012 The in vivo muscarinic receptor binding of antimuscarinic agents (oxybutynin, solifenacin, tolterodine, and imidafenacin) used to treat urinary dysfunction in patients with overactive bladder is reviewed.
Shizuo Yamada +3 more
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Brain Sciences, 2020 Ovarian hormones, such as estrogens and progesterone, are known to exert beneficial effects on cognition and some psychiatric disorders. The basis of these effects is not fully understood, but may involve altered cholinergic neurotransmission. This study
Sarah S. Ch’ng +9 more
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Antipsychotic-like effect of the muscarinic acetylcholine receptor agonist BuTAC in non-human primates. [PDF]
PLoS ONE, 2015 Cholinergic, muscarinic receptor agonists exhibit functional dopamine antagonism and muscarinic receptors have been suggested as possible future targets for the treatment of schizophrenia and drug abuse. The muscarinic ligand (5R,6R)-6-(3-butylthio-1,2,5-
Maibritt B Andersen +6 more
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Journal of Pharmacological Sciences, 2020 Cholinergic neurons play an important role in the higher functions of the brain, such as the memory, cognition, and nociception. However, the exact mechanism behind how the stimulation of all the muscarinic M1 receptors in the entire brain results in the
Keisuke Migita +7 more
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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 +5 more
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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 +3 more
core +1 more source
The role of muscarinic receptors in the beneficial effects of adenosine against myocardial reperfusion injury in rats. [PDF]
PLoS ONE, 2011 Adenosine, a catabolite of ATP, displays a wide variety of effects in the heart including regulation of cardiac response to myocardial ischemia and reperfusion injury.
Lei Sun +8 more
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