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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Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. [PDF]
, 2016 Pulmonary hypertension (PH) is a complex disease comprising a pathologic remodeling and thickening of the pulmonary vessels causing an after load on the right heart ventricle that can result in ventricular failure. Triggered by oxidative stress, episodes
Ahmed, Mohamed +5 more
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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 +4 more
doaj +1 more source
M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes [PDF]
, 2017 Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity.
Alvarez-Curto, Elisa +2 more
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Voltage Dependence of Muscarinic M1-,M3- and M5 Receptors [PDF]
Biophysical Journal, 2014 Muscarinic receptors (MR) are G protein-coupled receptors (GPCRs). Localized to the plasma membrane, they sense changes of the membrane potential and exhibit voltage-dependent signaling. Because voltage activates Gq-coupled receptors (e.g. M1R) but deactivates Gi-coupled receptors (e.g.
Moritz Bünemann +3 more
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Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]
, 2018 The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J. +14 more
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Journal 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
Journal of Pharmacological Sciences, 2016 The present study investigated pharmacological characterizations of muscarinic acetylcholine receptor (AChR) subtypes involving ACh-induced endothelium-independent vasodilatation in rat mesenteric arteries.
Panot Tangsucharit +6 more
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Allosteric interactions at the M3 muscarinic acetylcholine receptor
, 2023 The extracellular loops of muscarinic acetylcholine receptors are predicted to play a role in the binding and regulation of allosteric modulators. Furthermore, the sequence of the five subtypes of muscarinic receptors shows a large degree of diversity in this region.
openaire +4 more sources
Mir-34a-5p Mediates Cross-Talk between M2 Muscarinic Receptors and Notch-1/EGFR Pathways in U87MG Glioblastoma Cells: Implication in Cell Proliferation [PDF]
, 2018 Glioblastoma (GBM) is the most aggressive human brain tumor. The high growth potential and decreased susceptibility to apoptosis of the glioma cells is mainly dependent on genetic amplifications or mutations of oncogenic or pro-apoptotic genes ...
Bevilacqua, Valeria +8 more
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