Results 11 to 20 of about 13,431 (223)

The Role of Muscarinic Acetylcholine Receptor M₃ in Cardiovascular Diseases. [PDF]

Int J Mol Sci
The muscarinic acetylcholine receptor M3 (M3-mAChR) is involved in various physiological and pathological processes. Owing to specific cardioprotective effects, M3-mAChR is an ideal diagnostic and therapeutic biomarker for cardiovascular diseases (CVDs).
Liu X, Yu Y, Zhang H, Zhang M, Liu Y.
europepmc   +3 more sources

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of ¹⁸F-Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3. [PDF]

ChemMedChem
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Herrera-Rueda MA, Boateng MA, Wuest M, West FG, Wuest F.   +4 more
europepmc   +2 more sources

The M3 Muscarinic Acetylcholine Receptor Promotes Epidermal Differentiation

Journal of Investigative Dermatology, 2022
The M3 muscarinic acetylcholine receptor is predominantly expressed in the basal epidermal layer where it mediates the effects of the autocrine/paracrine cytotransmitter acetylcholine. Patients with the autoimmune blistering disease pemphigus develop autoantibodies to M3 muscarinic acetylcholine receptor and show alterations in keratinocyte adhesion ...
Junyan Duan, Charles Grando, Shuman Liu, Alex Chernyavsky, Jefferson K. Chen, Bogi Andersen, Sergei A. Grando   +6 more
openaire   +4 more sources

Expression of M3 muscarinic acetylcholine receptors in gastric cancer

Romanian Journal of Morphology and Embryology, 2022
Gastric cancer represents a real public health problem as far as incidence, aggressiveness and unfavorable prognosis are concerned. The autonomous nervous system might be one of the major factors involved in the onset, progression, and metastasis, both sympathetically and parasympathetically.
Mehedinţeanu, Alina Maria, Mirea, Cecil Sorin, Stovicek, Puiu Olivian, Schenker, Michael, Stancu, Marius Ionuţ, Ciurea, Ana-Maria, Streba, Liliana, Istrate-Ofiţeru, Anca-Maria, Sas, Teodor-Nicuşor, Vere, Cristin Constantin   +9 more
openaire   +2 more sources

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

Beneficial metabolic effects of M3 muscarinic acetylcholine receptor deficiency [PDF]

Cell Metabolism, 2006
Most animal models of obesity and hyperinsulinemia are associated with increased vagal cholinergic activity. The M3 muscarinic acetylcholine receptor subtype is widely expressed in the brain and peripheral tissues and plays a key role in mediating the physiological effects of vagal activation.
Gautam, Dinesh, Gavrilova, Oksana, Jeon, Jongrye, Pack, Stephanie, Jou, William, Cui, Yinghong, Li, Jian H., Wess, Jürgen   +7 more
openaire   +2 more sources

Novel Insights into M3 Muscarinic Acetylcholine Receptor Physiology and Structure [PDF]

Journal of Molecular Neuroscience, 2013
Recent studies with M3 muscarinic acetylcholine receptor (M3R) mutant mice suggest that drugs selectively targeting this receptor subtype may prove useful for the treatment of various pathophysiological conditions. Moreover, the use of M3R-based designer G protein-coupled receptors (GPCRs) has provided novel insights into how Gq-coupled GPCRs can ...
Andrew C, Kruse, Jianhua, Li, Jianxin, Hu, Brian K, Kobilka, Jürgen, Wess   +4 more
openaire   +2 more sources

Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists [PDF]

Proceedings of the National Academy of Sciences, 2018
Significance The development of selective antagonists for muscarinic acetylcholine receptors is challenging due to high homology in orthosteric binding sites among subtypes. Starting from a single amino acid difference in the orthosteric pockets in M2 muscarinic acetylcholine receptor (M2R) and M3R, we developed an M3R-selective antagonist ...
Liu, Hongtao, Hofmann, Josefa, Fish, Inbar, Schaake, Benjamin, Eitel, Katrin, Bartuschat, Amelie, Kaindl, Jonas, Rampp, Hannelore, Banerjee, Ashutosh, Hübner, Harald, Clark, Mary J, Vincent, Sandra G, Fisher, John T, Heinrich, Markus R, Hirata, Kunio, Liu, Xiangyu, Sunahara, Roger K, Shoichet, Brian K, Kobilka, Brian K, Gmeiner, Peter   +19 more
openaire   +4 more sources

M3 muscarinic acetylcholine receptor–reactive Th17 cells in primary Sjögren’s syndrome [PDF]

JCI Insight, 2020
M3 muscarinic acetylcholine receptor (M3R) is one of the autoantigens associated with Sjögren's syndrome (SS) and is localized in exocrine glands where disease-specific inflammation occurs. The inflammatory lesion is characterized by infiltration of CD4+ T cells, including clonally expanded Th17 cells.
Saori Abe, Hiroto Tsuboi, Hanae Kudo, Hiromitsu Asashima, Yuko Ono, Fumika Honda, Hiroyuki Takahashi, Mizuki Yagishita, Shinya Hagiwara, Yuya Kondo, Isao Matsumoto, Takayuki Sumida   +11 more
openaire   +2 more sources

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, Aslanoglou, Despoina, Marsango, Sara, Milligan, Graeme   +3 more
core   +1 more source