Results 21 to 30 of about 18,745 (209)

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., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

Identification and Molecular Characterization of m3 Muscarinic Receptor Dimers [PDF]

Journal of Biological Chemistry, 1999
Several studies suggest, but do not prove directly, that muscarinic receptors may be able to form dimeric or oligomeric arrays. To address this issue in a more direct fashion, we designed a series of biochemical experiments using a modified version of the rat m3 muscarinic receptor (referred to as m3') as a model system.
F Y, Zeng, J, Wess
openaire   +2 more sources

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, Lopez-Gimenez, Juan, Milligan, Graeme   +2 more
core   +1 more source

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

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, Yasuyuki Tanahashi, Takio Kitazawa, Masahisa Yamada, Seiichi Komori, Toshihiro Unno   +5 more
doaj   +1 more source

Inhibition of m3 muscarinic acetylcholine receptors by local anaesthetics [PDF]

British Journal of Pharmacology, 2001
Muscarinic m1 receptors are inhibited by local anaesthetics (LA) at nM concentrations. To elucidate in more detail the site(s) of LA interaction, we compared these findings with LA effects on m3 muscarinic receptors. We expressed receptors in Xenopus oocytes.
Hollmann, M. W., Ritter, C. H., Henle, P., de Klaver, M., Kamatchi, G. L., Durieux, M. E.   +5 more
openaire   +3 more sources

Identification and Role of Muscarinic Receptor Subtypes Expressed in Rat Adrenal Medullary Cells

Journal of Pharmacological Sciences, 2011
.: The muscarinic receptor is known to be involved in the acetylcholine (ACh)-induced secretion of catecholamines in the adrenal medullary (AM) cells of various mammals.
Keita Harada, Hidetada Matsuoka, Takeyoshi Sata, Akira Warashina, Masumi Inoue   +4 more
doaj   +1 more source

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, Caffarelli, Elisa, De Jaco, Antonella, Di Bari, Maria, Laneve, Pietro, Piovesana, Roberta, Talora, Claudio, Tata, Ada Maria, Trobiani, Laura   +8 more
core   +2 more sources

Structural Basis of M3 Muscarinic Receptor Dimer/Oligomer Formation [PDF]

Journal of Biological Chemistry, 2011
Class A G protein-coupled receptors (GPCRs) are known to form dimers and/or oligomeric arrays in vitro and in vivo. These complexes are thought to play important roles in modulating class A GPCR function. Many studies suggest that residues located on the "outer" (lipid-facing) surface of the transmembrane (TM) receptor core are critically involved in ...
Sara M, McMillin, Moritz, Heusel, Tong, Liu, Stefano, Costanzi, Jürgen, Wess   +4 more
openaire   +2 more sources

Muscarinic acetylcholine receptor M1 and M3 subtypes mediate acetylcholine-induced endothelium-independent vasodilatation in rat mesenteric arteries

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, Shingo Takatori, Yoshito Zamami, Mitsuhiro Goda, Poungrat Pakdeechote, Hiromu Kawasaki, Fusako Takayama   +6 more
doaj   +1 more source

Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation [PDF]

, 2007
Recent studies suggest that the second extracellular loop (o2 loop) of bovine rhodopsin and other class I G protein-coupled receptors (GPCRs) targeted by biogenic amine ligands folds deeply into the transmembrane receptor core where the binding of cis ...
Kim, Soo-Kyung, Li, Bo, Scarselli, Marco, Wess, Jürgen   +3 more
core   +1 more source