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+4 more
doaj +1 more source
M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes [PDF]
Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity.
Alvarez-Curto, Elisa+2 more
core +1 more source
Muscarinic modulation of M and h currents in gerbil spherical bushy cells.
Descending cholinergic fibers innervate the cochlear nucleus. Spherical bushy cells, principal neurons of the anterior part of the ventral cochlear nucleus, are depolarized by cholinergic agonists on two different time scales.
Charlène Gillet+2 more
doaj +1 more source
Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]
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+3 more
core +2 more sources
Assessing the clinical value of fast onset and sustained duration of action of long-acting bronchodilators for COPD [PDF]
Date of Aceptance: 12/02/2015 Acknowledgments The authors were assisted in the preparation of the manuscript by Sarah Filcek, a professional medical writer at CircleScience (Tytherington, UK), part of KnowledgePoint360, an Ashfield Company.
Beeh, Kai M+3 more
core +1 more source
Light-Activated Pharmacological Tools for Exploring the Cholinergic System. [PDF]
ABSTRACT Cholinergic transmission plays a critical role in both the central and peripheral nervous systems, affecting processes such as learning, memory, and inflammation. Conventional cholinergic drugs generally suffer from poor selectivity and temporal precision, leading to undesired effects and limited therapeutic efficacy. Photopharmacology aims to
Colleoni A+5 more
europepmc +2 more sources
Geometry of muscarinic agonists.
In order to account for a common geometric character of the skeleton of known muscarinic agonist molecules in the drug-receptor interaction, common key atoms, terminal methyl carbon, two oxygen, and ammonium nitrogen atoms were remarked which were shown by computer calculation to be concentrated at definite points in space and to be arranged nearly in ...
openaire +4 more sources
Simultaneous release of glutamate and acetylcholine from single magnocellular "cholinergic" basal forebrain neurons [PDF]
Basal forebrain (BF) neurons provide the principal cholinergic drive to the hippocampus and cortex. Their degeneration is associated with the cognitive defects of Alzheimer's disease. Immunohistochemical studies suggest that some of these neurons contain
Abogadie, FC, Allen, TGJ, Brown, DA
core +1 more source
Altered muscarinic and nicotinic receptor densities in cortical and subcortical brain regions in Parkinson's disease [PDF]
Muscarinic and nicotinic cholinergic receptors and choline acetyltransferase activity were studied in postmortem brain tissue from patients with histopathologically confirmed Parkinson's disease and matched control subjects.
Jenner, P.+3 more
core +1 more source
The Association Between Urinary Tract Infection and Overactive Bladder Treatment
Background: Overactive bladder (OAB) syndrome is defined as urinary urgency, with or without urge incontinence in the absence of an underlying pathological or metabolic cause.
Kuang-Ming Liao+7 more
doaj +1 more source