M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes [PDF]
, 2017 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
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Interaction of the Xanthine Nucleotide Binding Goα Mutant with G Protein-coupled Receptors [PDF]
, 1998 We constructed a double mutant version of the α subunit of Go that was regulated by xanthine nucleotides instead of guanine nucleotides (GoαX). We investigated the interaction between GoαX and G protein-coupled receptors in vitro.
Simon, Melvin I., Yu, Bo
core +1 more source
Time Course of the Increase in the Myocardial Slow Inward Current after a Photochemically Generated Concentration Jump of Intracellular cAMP [PDF]
, 1983 Voltage-clamped atrial trabeculae from bullfrog hearts were exposed to membrane-permeant photolyzable o-nitrobenzyl esters of cAMP and cGMP. UV flashes produced intracellular concentration jumps of cAMP or cGMP. With the cAMP derivative, flashes resulted
Engels, Joachim +3 more
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Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogenous time-resolved FRET [PDF]
, 2010 Flp-In T-REx 293 cells expressing a wild type human M muscarinic acetylcholine receptor construct constitutively and able to express a Receptor Activated Solely by Synthetic Ligand (RASSL) form of this receptor on demand maintained response to the ...
Alvarez-Curto, Elisa +3 more
core +2 more sources
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
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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
Muscarinic modulation of M and h currents in gerbil spherical bushy cells.
PLoS ONE, 2020 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
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Anticholinergic therapy for acute asthma in children. [PDF]
, 2012 Inhaled anticholinergics as single agent bronchodilators (or in combination with beta(2)-agonists) are one of the several medications available for the treatment of acute asthma in ...
Beakes +49 more
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LABA/LAMA combinations versus LAMA monotherapy or LABA/ICS in COPD : a systematic review and meta-analysis [PDF]
, 2017 Acknowledgments The meta-analysis work was performed by Guruprasad Rao KS and Sharanbasappa Durg of Molecular Connections (P) Ltd, Bangalore, India, under the guidance of the manuscript authors and Novartis Pharma AG (Basel, Switzerland). Medical writing
Altman, Pablo +8 more
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The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]
, 2013 G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D. +2 more
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