Results 31 to 40 of about 687,004 (308)

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie, Schaller, David, Stark, Holger, Wolber, Gerhard   +3 more
core   +2 more sources

Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists

Proceedings of the National Academy of Sciences of the United States of America, 2018
Significance The development of selective antagonists for muscarinic acetylcholine receptors is challenging due to high homology in orthosteric binding sites among subtypes.
Hongtao Liu, J. Hofmann, I. Fish, B. Schaake, K. Eitel, A. Bartuschat, J. Kaindl, H. Rampp, A. Banerjee, H. Hübner, M. Clark, S. Vincent, J. Fisher, M. Heinrich, K. Hirata, Xiangyu Liu, R. Sunahara, B. Shoichet, B. Kobilka, P. Gmeiner   +19 more
semanticscholar   +1 more source

Molecular probes for muscarinic receptors: Functionalized congeners of selective muscarinic antagonists [PDF]

Life Sciences, 1995
The muscarinic agonist oxotremorine and the tricyclic muscarinic antagonists pirenzepine and telenzepine have been derivatized using a functionalized congener approach for the purpose of synthesizing high affinity ligand probes that are suitable for conjugation with prosthetic groups, for receptor cross-linking, fluorescent and radioactive detection ...
K A, Jacobson, B, Fischer, A M, van Rhee
openaire   +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

Striatal cholinergic interneurons generate beta and gamma oscillations in the corticostriatal circuit and produce motor deficits [PDF]

, 2016
Cortico-basal ganglia-thalamic (CBT) neural circuits are critical modulators of cognitive and motor function. When compromised, these circuits contribute to neurological and psychiatric disorders, such as Parkinson's disease (PD).
Bucklin, Mark, Han, Xue, Kondabolu, Krishnakanth, Kopell, Nancy, McCarthy, Michelle M., Roberts, Erik A.   +5 more
core   +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

Neuropharmacological targets for drug action in vestibular sensory pathways [PDF]

, 2017
The use of pharmacological agents is often the preferred approach to the management of vestibular dysfunction. In the vestibular sensory pathways, the sensory neuroepithelia are thought to be influenced by a diverse number of neuroactive substances that ...
Jones, Timothy A, Lee, Choongheon
core   +3 more sources

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