ArticleThe Journal of physiology2003
Activation and block of mouse muscle-type nicotinic receptors by tetraethylammonium.
Article in The Journal of physiology, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 31 citations in OpenAlex.
- Endothelium-derived hyperpolarizing factor mediates bradykinin-stimulated tissue plasminogen activator release in humans.Journal of vascular research · 2014Trial
- Null method to estimate the maximal PA at subsaturating concentrations of agonist.The Journal of general physiology · 2025Article
- Crystal structure of the tetra-ethyl-ammonium salt of the non-steroidal anti-inflammatory drug nimesulide (polymorph II).Acta crystallographica. Section E, Crystallographic communications · 2024Article
- The synthesis, thermal behaviour, spectral and structural characterization, and in silico prediction of pharmacokinetic parameters of tetraalkylammonium salts of non-steroidal anti-inflammatory drug nimesulide.Scientific reports · 2023Article
- Isoform-specific mechanisms of α3β4*-nicotinic acetylcholine receptor modulation by the prototoxin lynx1.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2017Article
- Muscle-Type Nicotinic Receptor Modulation by 2,6-Dimethylaniline, a Molecule Resembling the Hydrophobic Moiety of Lidocaine.Frontiers in molecular neuroscience · 2016Article
- The atypical cation-conduction and gating properties of ELIC underscore the marked functional versatility of the pentameric ligand-gated ion-channel fold.The Journal of general physiology · 2015Article
- Poly(ethylene glycol) as a scaffold for high-affinity open-channel blockers of the mouse nicotinic acetylcholine receptor.PloS one · 2014Article
- Energy for wild-type acetylcholine receptor channel gating from different choline derivatives.Biophysical journal · 2013Article
- Functional characterization of the α5(Asn398) variant associated with risk for nicotine dependence in the α3β4α5 nicotinic receptor.Molecular pharmacology · 2011Article
- The activation mechanism of alpha1beta2gamma2S and alpha3beta3gamma2S GABAA receptors.The Journal of general physiology · 2010Article
- Agonist and blocking actions of choline and tetramethylammonium on human muscle acetylcholine receptors.The Journal of physiology · 2009Article
- A novel signaling pathway: fibroblast nicotinic receptor alpha1 binds urokinase and promotes renal fibrosis.The Journal of biological chemistry · 2009Article
- Probing protein packing surrounding the residues in and flanking the nicotinic acetylcholine receptor M2M3 loop.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2009Article
- Activation and block of the adult muscle-type nicotinic receptor by physostigmine: single-channel studies.Molecular pharmacology · 2008Article
- Diverse inhibitory actions of quaternary ammonium cholinesterase inhibitors on Torpedo nicotinic ACh receptors transplanted to Xenopus oocytes.British journal of pharmacology · 2007Article
- Block of muscle nicotinic receptors by choline suggests that the activation and desensitization gates act as distinct molecular entities.The Journal of general physiology · 2006Article
- Activation of heteroliganded mouse muscle nicotinic receptors.The Journal of physiology · 2005Article
- Galantamine activates muscle-type nicotinic acetylcholine receptors without binding to the acetylcholine-binding site.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2005Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
We have studied the activation and inhibition of the mouse muscle adult-type nicotinic acetylcholine receptor by tetraethylammonium (TEA) and related quaternary ammonium derivatives. The data show that TEA is a weak agonist of the nicotinic receptor. No single-channel clusters were observed at concentrations as high as 5 mM TEA or in the presence of a mutation which selectively increases the efficacy of the receptor. When coapplied with 1 mM carbamylcholine (CCh), TEA decreased the effective opening rate demonstrating that it acts as a competitive antagonist of CCh-mediated activation. Kinetic analysis of currents elicited by CCh and TEA allowed an estimate of receptor affinity for TEA of about 1 mM, while an upper limit of 10 s-1 could be set for the wild-type channel-opening rate constant for receptors activated by TEA alone. At millimolar concentrations, TEA inhibited nicotinic receptor currents by depressing the single-channel amplitude. The effect had an IC50 of 2-3 mM, depending on the conditions of the experiment, and resembled a standard open-channel block. However, the decrease in channel amplitudes was not accompanied by an increase in the mean burst duration, indicating that a linear open-channel blocking mechanism is not applicable. Upon studying block by other nicotinic receptor ligands it was found that block by CCh, tetramethylammonium and phenyltrimethylammonium can be accounted for by the sequential blocking mechanism while block in the presence of methyltriethylammonium, ethyltrimethylammonium or choline was inconsistent with such a mechanism. A mechanism in which receptors blocked by TEA can close would account for the experimental findings.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.