Results 121 to 130 of about 28,480 (301)
Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation [PDF]
, 2007 Recent studies suggest that the second extracellular loop (o2 loop) of bovine rhodopsin and other class I G protein-coupled receptors (GPCRs) targeted by biogenic amine ligands folds deeply into the transmembrane receptor core where the binding of cis ...
Kim, Soo-Kyung +3 more
core +1 more source
British Journal of Pharmacology, Volume 182, Issue 11, Page 2487-2502, June 2025.Background and Purpose Hyoscine butylbromide (HBB) has a low oral (PO) bioavailability. Further, limited data on its activity on non‐gastrointestinal (GI) smooth muscle spasms after oral dosing are available, causing its effects beyond the GI tract to be questioned.
Sara Traserra +4 more
wiley +1 more source
Frontiers in Cellular Neuroscience, 2019 In hippocampal CA1, muscarinic acetylcholine (ACh) receptor (mAChR) activation via exogenous application of cholinergic agonists has been shown to presynaptically inhibit Schaffer collateral (SC) glutamatergic inputs in stratum radiatum (SR), and ...
Priyodarshan Goswamee, A. Rory McQuiston
doaj +1 more source
PET mapping of receptor occupancy using joint direct parametric reconstruction [PDF]
Receptor occupancy (RO) studies using PET neuroimaging play a critical role in the development of drugs targeting the central nervous system (CNS). The conventional approach to estimate drug receptor occupancy consists in estimation of binding potential changes between two PET scans (baseline and post-drug injection).
arxiv +1 more source
Simultaneous Modeling of In Vivo and In Vitro Effects of Nondepolarizing Neuromuscular Blocking Drugs [PDF]
arXiv, 2023 Nondepolarizing neuromuscular blocking drugs (NDNBs) are clinically used to produce muscle relaxation during general anesthesia. This paper explores a suitable model structure to simultaneously describe in vivo and in vitro effects of three clinically used NDNBs, cisatracurium, vecuronium, and rocuronium. In particular, it is discussed how to reconcile
arxiv
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
Generation of an agonistic binding site for blockers of the M3 muscarinic acetylcholine receptor [PDF]
Biochemical Journal, 2008 GPCRs (G-protein-coupled receptors) exist in a spontaneous equilibrium between active and inactive conformations that are stabilized by agonists and inverse agonists respectively. Because ligand binding of agonists and inverse agonists often occurs in a competitive manner, one can assume an overlap between both binding sites.
Angela Schulz +3 more
openaire +3 more sources
Cholesterol modulates acetylcholine receptor diffusion by tuning confinement sojourns and nanocluster stability [PDF]
arXiv, 2017 Translational motion of neurotransmitter receptors is key for determining receptor number at the synapse and hence, synaptic efficacy. We combine live-cell STORM superresolution microscopy of nicotinic acetylcholine receptor (nAChR) with single-particle tracking, mean-squared displacement (MSD), turning angle, ergodicity, and clustering analyses to ...
arxiv
Autoantibodies against Muscarinic Acetylcholine Receptor on Exocrine Glands in Sjögren Syndrome [PDF]
, 2014 These investigations demonstrate that serum antibodies against muscarinic acetylcholine receptors (mAChR) in primary Sjögren syndrome (pSS) and associated Sjögren syndrome (aSS) bind and activate both cholinergic receptors of M3 in salivary gland and M1 ...
Borda, Enri Santiago +1 more
core +1 more source
Investigative Ophthalmology and Visual Science, 2014 PURPOSE We tested the hypothesis that the M3 muscarinic acetylcholine receptor subtype mediates cholinergic responses in murine ophthalmic arteries after endothelial removal.
Adrian Gericke +5 more
semanticscholar +1 more source