Results 21 to 30 of about 149,769 (206)

Discovery of Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists

, 2016
High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity.
Kristen E. Belmonte (2415082), Yonghui Wang (287491), Roderick S. Davis (2422657), James J. Foley (2378872), Chris J. Dehaas (2422654), Michael Salmon (2353963), Dwight M. Morrow (2415079), Dongchuan Shi (2259844), Ralph A. Rivero (1993048), Parvathi Rao (2259841), Lorena A. Kallal (440592), Jian Jin (351142), Miriam Burman (2353924), Qi Jin (12159), Michael L. Moore (1993054), Michael Palovich (2232403), Feng Wang (44414), Edward F. Webb (2353930), Henry M. Sarau (2353933), Jakob Busch-Petersen (2353945), Wei Fu (176366), Manuela Berlanga (650252)   +21 more
core   +2 more sources

Molecular Basis for Activation to Inhibition Switching in Kv7.2 Channel Modulators

Angewandte Chemie, EarlyView.
The paper describes the serendipitous discovery of chemical manipulation allowing the activator‐to‐inhibitor switching in Kv7.2 channel modulators. The molecular determinants driving this switch have been rationalized by multidisciplinary investigation encompassing synthetic and analytical chemistry, in silico methods, cryo‐EM analysis ...
Tania Ciaglia, Giusy Carleo, Zhenni Yang, Francesca Di Matteo, Federica De Rosa, Gerardina Smaldone, Zhao‐Bing Gao, Marco D'Alì, Rita Turcio, Demin Ma, Veronica Di Sarno, Nannan Su, Salvatore Vincenzo Giofrè, Giacomo Pepe, Pietro Campiglia, Alessia Bertamino, Francesco Miceli, Jiangtao Guo, Nunzio Iraci, Carmine Ostacolo, Maurizio Taglialatela   +20 more
wiley   +2 more sources

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

Clinical predictors of treatment response to tiotropium add-on therapy in adult asthmatic patients: From multicenter real-world cohort data in Korea

World Allergy Organization Journal, 2022
Background: Tiotropium, a long-acting muscarinic antagonist, is recommended for add-on therapy to inhaled corticosteroids (ICS)-long-acting beta 2 agonists (LABA) for severe asthma.
Ji-Su Shim, MD, PhD, Juhae Jin, MA, Sae-Hoon Kim, MD, PhD, Taehoon Lee, MD, PhD, An-Soo Jang, MD, PhD, Chan Sun Park, MD, PhD, Jae-Woo Jung, MD, PhD, Jae-Woo Kwon, MD, PhD, Ji-Yong Moon, MD, PhD, Min-Suk Yang, MD, PhD, Jaechun Lee, MD, PhD, Jeong-Hee Choi, MD, PhD, Yoo Seob Shin, MD, PhD, Hee-Kyoo Kim, MD, PhD, Sujeong Kim, MD, PhD, Joo-Hee Kim, MD, PhD, Sang-Heon Cho, MD, PhD, Young-Hee Nam, MD, PhD, Sang-Hoon Kim, MD, PhD, So Young Park, MD, PhD, Gyu Young Hur, MD, PhD, Sang-Ha Kim, MD, PhD, Hye-Kyung Park, MD, PhD, Hyun Jung Jin, MD, PhD, Jae-Hyun Lee, MD, PhD, Jung-Won Park, MD, PhD, Ho Joo Yoon, MD, PhD, Byoung Whui Choi, MD, PhD, Young-Joo Cho, MD, PhD, Min-Hye Kim, MD, PhD, Tae-Bum Kim, MD, PhD   +30 more
doaj   +1 more source

Dementia patients have greater anti-cholinergic drug burden on discharge from hospital: A multicentre cross-sectional study

European Psychiatry, 2021
Introduction Anticholinergic medications block cholinergic transmission. The central effects of anticholinergic drugs can be particularly marked in patients with dementia.
J. Randall, A. Hook, C-M. Grubb, N. Ellis, J. Wellington, A. Hemmad, A. Zerdelis, B. Geers, B. Sykes, C. Auty, C. Vinchenzo, C. Thorburn, D. Asogbon, E. Granger, H. Boagey, J. Raphael, K. Patel, K. Bhargava, M.-K. Dolley, M. Maden, M. Shah, Q. Lee, R. Vaidya, S. Sehdev, S. Barai, S. Roche, U. Khalid, J. Harrison, D. Codling   +28 more
doaj   +1 more source