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 +3 more
core +2 more sources
Evidence for Respiratory Neuromodulator Interdependence after Cholinergic Disruption in the Ventral Respiratory Column [PDF]
, 2015 Reverse dialysis of the muscarinic receptor antagonist, atropine (ATR, 50 mM), into the pre-Bötzinger Complex region of the ventral respiratory column (VRC) of awake and sleeping goats increases breathing frequency and serotonin (5-HT), substance P (SP),
Forster, Hubert +6 more
core +2 more sources
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. +3 more
core +1 more source
Identification of atropine-and P2X1 receptor antagonist-reistant, neurogenic contractions of the urinary bladder [PDF]
, 2007 Acetylcholine and ATP are excitatory cotransmitters in parasympathetic nerves. We used P2X1 receptor antagonists to further characterize the purinergic component of neurotransmission in isolated detrusor muscle of guinea pig urinary bladder.
Gallagher, Gemma +3 more
core +1 more source
Molecular Cages as Probes in Indicator Displacement Assays: The Case of Scopolamine Detection
Angewandte Chemie, EarlyView.In this research, we show the concept of molecular cages as probes in indicator displacement assays, focusing on scopolamine detection, a drug often used in drug‐facilitated sexual assaults. Drug sensing occurs via the drug‐induced transformation of non‐emissive [Fluorescein2⊂Cage] complex into [Scopolamine⊂Catenane] and highly emissive free ...
Giovanni Montà‐González +5 more
wiley +2 more sources
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 +11 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 +5 more
core +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
Is there a rationale and role for long-acting anticholinergic bronchodilators in asthma? [PDF]
, 2014 The authors acknowledge the medical writing assistance received from Sam Yarwood, PhD, of Complete HealthVizion, in the form of literature searches and preparation and revision of the draft manuscript.Peer reviewedPublisher ...
Fromer, Leonard +4 more
core +10 more sources
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 +4 more
doaj +1 more source