ArticleBritish journal of pharmacology2010
The neuronal nicotinic alpha4beta2 receptor has a high maximal probability of being open.
Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 41 citations in OpenAlex.
- Structural mechanism of lipid modulation of pentameric ligand-gated ion channel activity.bioRxiv : the preprint server for biology · 2025Article
- Nicotine: From Discovery to Biological Effects.International journal of molecular sciences · 2023Review
- Structure and Function of the Mammalian Neuromuscular Junction.Comprehensive Physiology · 2022Article
- Nicotinic Acetylcholine Receptor Accessory Subunits Determine the Activity Profile of Epibatidine Derivatives.Molecular pharmacology · 2020Article
- More than Smoke and Patches: The Quest for Pharmacotherapies to Treat Tobacco Use Disorder.Pharmacological reviews · 2020Review
- Heteromeric Neuronal Nicotinic Acetylcholine Receptors with MutantThe Journal of pharmacology and experimental therapeutics · 2019Article
- A tale of ligands big and small: an update on how pentameric ligand-gated ion channels interact with agonists and proteins.Current opinion in physiology · 2019Article
- Cellular, Synaptic and Network Effects of Acetylcholine in the Neocortex.Frontiers in neural circuits · 2019Review
- 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
- Article
- Introduced Amino Terminal Epitopes Can Reduce Surface Expression of Neuronal Nicotinic Receptors.PloS one · 2016Article
- Intramembrane aromatic interactions influence the lipid sensitivities of pentameric ligand-gated ion channels.The Journal of biological chemistry · 2015Article
- Merging old and new perspectives on nicotinic acetylcholine receptors.Biochemical pharmacology · 2014Review
- A distinct mechanism for activating uncoupled nicotinic acetylcholine receptors.Nature chemical biology · 2013Article
- Molecular mechanisms of acetylcholine receptor-lipid interactions: from model membranes to human biology.Biophysical reviews · 2013Review
- Intrinsically low open probability of α7 nicotinic acetylcholine receptors can be overcome by positive allosteric modulation and serum factors leading to the generation of excitotoxic currents at physiological temperatures.Molecular pharmacology · 2012Article
- The nicotinic acetylcholine receptors of zebrafish and an evaluation of pharmacological tools used for their study.Biochemical pharmacology · 2012Article
- Characterizing low affinity epibatidine binding to α4β2 nicotinic acetylcholine receptors with ligand depletion and nonspecific binding.BMC biophysics · 2011Article
- Characterizing functional α6β2 nicotinic acetylcholine receptors in vitro: mutant β2 subunits improve membrane expression, and fluorescent proteins reveal responsive cells.Biochemical pharmacology · 2011Article
- Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.Biochemical pharmacology · 2011Review
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2 authors at 1 institution in 1 country.
Funding
Abstract
background and purposeA fundamental property of transmitter-gated ion channels is the probability a channel will be open (P(open)) when stimulated by a concentration of agonist that elicits a maximal response. This value is critical for interpreting steady-state concentration-response relationships in terms of channel activation, and for understanding the actions of drugs that potentiate responses. We used analysis of non-stationary noise to estimate the maximal probability the nicotinic alpha4beta2 receptor is open. EXPERIMENTAL APPROACH: HEK293 cells stably transfected to express human alpha4beta2 nicotinic receptors were studied using whole-cell voltage clamp. Nicotinic agonists (acetylcholine, nicotine, cytisine and 5-iodo A-85380) were applied, and the relationship between variance of the elicited whole-cell current and mean current was analysed. KEY
resultsThe variance did not increase linearly with the mean current. For acetylcholine and nicotine the relationship between variance and mean indicates that the maximal P(open) is greater than 0.8. The number of agonist-activatable channels was estimated to be about 1000 per cell. The mean single channel conductance at -60 mV was indistinguishable when currents were elicited by acetylcholine (18 pS), nicotine (17 pS) or 5-iodo A-85380 (17 pS), whereas the value for cytisine was larger (24 pS). CONCLUSIONS AND IMPLICATIONS: The neuronal nicotinic alpha4beta2 receptor has a maximal probability of being open that is greater than 0.8. This conclusion applies to the receptor containing three alpha4 and two beta2 subunits (the low-sensitivity stoichiometry), but may not apply to the receptor containing two alpha4 and three beta2 subunits (the high-sensitivity stoichiometry).
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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.