Results 21 to 30 of about 687,004 (308)

Selective M3 Muscarinic Receptor Antagonist Inhibits Small-Cell Lung Carcinoma Growth in a Mouse Orthotopic Xenograft Model

Journal of Pharmacological Sciences, 2011
.: In small cell lung carcinoma (SCLC), acetylcholine (ACh) is synthesized and secreted, and it acts as an autocrine growth factor through activation of its receptors, muscarinic receptor (mAChR) and nicotinic receptor (nAChR). Alteration of tumor growth
Nozomi Ami, Kazumi Koga, Hiroshi Fushiki, Yoko Ueno, Yoshio Ogino, Hisashi Ohta   +5 more
doaj   +1 more source

Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs [PDF]

, 2016
Although rhodopsin-like G protein-coupled receptors can exist as both monomers and non-covalently associated dimers/oligomers, the steady-state proportion of each form and whether this is regulated by receptor ligands is unknown.
Godin, Antoine G., Marsango, Sara, Milligan, Graeme, Pediani, John D., Ward, Richard J.   +4 more
core   +1 more source

Muscarinic Acetylcholine Type 1 Receptor Activity Constrains Neurite Outgrowth by Inhibiting Microtubule Polymerization and Mitochondrial Trafficking in Adult Sensory Neurons

Frontiers in Neuroscience, 2018
The muscarinic acetylcholine type 1 receptor (M1R) is a metabotropic G protein-coupled receptor. Knockout of M1R or exposure to selective or specific receptor antagonists elevates neurite outgrowth in adult sensory neurons and is therapeutic in diverse ...
Mohammad G. Sabbir, Nigel A. Calcutt, Paul Fernyhough, Paul Fernyhough   +3 more
doaj   +1 more source

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, Al-Abed, Yousef, Coleman, Thomas, Lakshminrusimha, Satyanarayana, Patel, Hardik, VanPatten, Sonya   +5 more
core   +2 more sources

Inhaled corticosteroids with combination inhaled long-acting beta2-agonists and long-acting muscarinic antagonists for chronic obstructive pulmonary disease.

Cochrane Database of Systematic Reviews, 2016
BACKGROUND Management of chronic obstructive pulmonary disease (COPD) commonly involves long-acting bronchodilators including beta-agonists (LABA) and muscarinic antagonists (LAMA).
Daniel J Tan, Clinton J White, J. Walters, E. Walters   +3 more
semanticscholar   +1 more source

Combined Unilateral Blockade of Cholinergic, Peptidergic, And Serotonergic Receptors in The Ventral Respiratory Column Does Not Affect Breathing in Awake Or Sleeping Goats [PDF]

, 2015
Previous work in intact awake and sleeping goats has found that unilateral blockade of excitatory inputs in the ventral respiratory column (VRC) elicits changes in the concentrations of multiple neurochemicals, including serotonin (5-HT), substance P ...
Forster, Hubert, Hodges, Matthew, Langer, Thomas, Miller, Justin Robert, Muere, Clarissa, Neumueller, Suzanne, Olesiak, Samantha, Pan, Lawrence   +7 more
core   +2 more sources

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor

Proceedings of the National Academy of Sciences of the United States of America, 2018
Significance The orthosteric binding sites of the five muscarinic acetylcholine receptor (mAChR) subtypes are highly conserved, making the development of selective antagonists challenging.
M. Korczynska, M. Clark, C. Valant, Jun Xu, Ee Von Moo, Sabine Albold, Dahlia R. Weiss, Hayarpi Torosyan, Weijiao Huang, A. Kruse, B. Lyda, L. May, Joanne Baltos, P. Sexton, B. Kobilka, A. Christopoulos, B. Shoichet, R. Sunahara   +17 more
semanticscholar   +1 more source

The structural study of mutation-induced inactivation of human muscarinic receptor M4

IUCrJ, 2020
Human muscarinic receptor M4 belongs to the class A subfamily of the G-protein-coupled receptors (GPCRs). M4 has emerged as an attractive drug target for the treatment of Alzheimer's disease and schizophrenia.
Jingjing Wang, Meng Wu, Lijie Wu, Yueming Xu, Fei Li, Yiran Wu, Petr Popov, Lin Wang, Fang Bai, Suwen Zhao, Zhi-Jie Liu, Tian Hua   +11 more
doaj   +1 more source

Myopia-Inhibiting Concentrations of Muscarinic Receptor Antagonists Block Activation of Alpha2A-Adrenoceptors In Vitro.

Investigative Ophthalmology and Visual Science, 2018
Purpose Myopia is a refractive disorder that degrades vision. It can be treated with atropine, a muscarinic acetylcholine receptor (mAChR) antagonist, but the mechanism is unknown. Atropine may block α-adrenoceptors at concentrations ≥0.1 mM, and another
Brittany J. Carr, K. Mihara, R. Ramachandran, M. Saifeddine, N. Nathanson, W. Stell, M. Hollenberg   +6 more
semanticscholar   +1 more source

Carbachol increases intracellular free calcium concentrations in human granulosa-lutein cells [PDF]

, 1992
We investigated whether the stimulation of human granulosa-lutein cells with muscarinic and nicotinic receptor agonists can cause increases in intracellular free calcium (Ca2+), using Fura-2 microfluorimetry.
Föhr, K. J., Gratzl, Manfred, Mayerhofer, Artur, Sterzik, K.   +3 more
core   +1 more source