Results 11 to 20 of about 22,543 (220)

Investigating the Unbinding of Muscarinic Antagonists from the Muscarinic 3 Receptor. [PDF]

J Chem Theory Comput, 2023
Patient symptom relief is often heavily influenced by the residence time of the inhibitor-target complex. For the human muscarinic receptor 3 (hMR3), tiotropium is a long-acting bronchodilator used in conditions such as asthma or chronic obstructive pulmonary disease (COPD). The mechanistic insights into this inhibitor remain unclear; specifically, the
Buigues PJ, Gehrke S, Badaoui M, Dudas B, Mandana G, Qi T, Bottegoni G, Rosta E.   +7 more
europepmc   +4 more sources

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

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

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

Combination therapy with indacaterol and glycopyrronium bromide in the management of COPD: an update on the evidence for efficacy and safety

Therapeutic Advances in Respiratory Disease, 2015
The international guidelines on chronic obstructive pulmonary disease (COPD) recommend inhaled bronchodilators for maintenance treatment of the disease. These drugs include β2-agonists and muscarinic antagonists, which are both available as short-acting ...
Erminia Ridolo, Marcello Montagni, Gian Galeazzo Riario-Sforza, Marco Baroni, Cristoforo Incorvaia   +4 more
doaj   +1 more source

Single Inhaler LABA/LAMA for COPD

Frontiers in Pharmacology, 2019
Chronic obstructive pulmonary disease (COPD) is a common disabling disease characterized by progressive airflow obstruction. Great efforts were spent in the development of drugs able to improve symptoms, quality of life, reduce exacerbations ...
Mario Malerba, Mario Malerba, Valentina Foci, Valentina Foci, Filippo Patrucco, Filippo Patrucco, Patrizia Pochetti, Patrizia Pochetti, Matteo Nardin, Corrado Pelaia, Alessandro Radaeli   +10 more
doaj   +1 more source

Muscarinic M1 receptors stimulated by intracerebroventricular administration of McN-A-343 reduces the nerve injury-induced mechanical hypersensitivity via GABAB receptors rather than GABAA receptors in mice

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, Akiko Nishimura, Fumihiro Eto, Kohei Koga, Taichi Matsumoto, Kazuki Terada, Shuji Hara, Kenji Honda   +7 more
doaj   +1 more source

Muscarinic Receptor Subtypes Mediating Positive and Negative Inotropy in the Developing Chick Ventricle

Journal of Pharmacological Sciences, 2007
The inotropic response to muscarinic receptor stimulation of isolated chick ventricular myocardium was examined at various developmental stages, and the receptor subtype involved was pharmacologically characterized.
Hideaki Nouchi, Seri Kaeriyama, Akiko Muramatsu, Masumi Sato, Kunihiko Hirose, Nagako Shimizu, Hikaru Tanaka, Koki Shigenobu   +7 more
doaj   +1 more source

The Bronchoprotective Effects of Dual Pharmacology, Muscarinic Receptor Antagonist and β₂ Adrenergic Receptor Agonist Navafenterol in Human Small Airways

Cells, 2023
Bronchodilators and anti-inflammatory agents are the mainstream treatments in chronic obstructive and pulmonary disease (COPD) and asthma.
Joseph Antony Jude, Ian Dainty, Nikhil Karmacharya, William Jester, Reynold Panettieri   +4 more
doaj   +1 more source

Characterization of Prejunctional Muscarinic Receptors: Effects on the Release of VIP and Functional Responses and Receptor Expression in the Ovine Submandibular Gland

Advances in Pharmacological Sciences, 2009
In the in vivo experiments on anaesthetized sheep, it was presently examined whether muscarinic receptor antagonists with diverse selectivity affect the release of VIP in response to electrical stimulation of the parasympathetic chorda tympanic nerve ...
Anders T. Ryberg, Ondrej Soukup, Gunnar Tobin   +2 more
doaj   +1 more source