ArticleMethods in molecular biology (Clifton, N.J.)2012
Mutations in the GABAA receptor that mimic the allosteric ligand etomidate.
Article in Methods in molecular biology (Clifton, N.J.), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 17 citations in OpenAlex.
- Glabridin Hypnosis in Zebrafish Larvae Is Associated With Effects on Multiple Anesthetic Target Receptors.Anesthesia and analgesia · 2025Article
- Article
- Substituted Cysteine Modification and Protection with n-Alkyl-MTS Reagents Quantifies Steric Changes Induced by a Mutation in Anesthetic Binding Sites on GABA Type A Receptors.Molecular pharmacology · 2023Article
- Perspective on the Relationship between GABAA Receptor Activity and the Apparent Potency of an Inhibitor.Current neuropharmacology · 2022Article
- Substituted Cysteine Modification and Protection withMolecular pharmacology · 2021Article
- Steady-state activation of the high-affinity isoform of the α4β2δ GABAScientific reports · 2019Article
- Steady-state activation and modulation of the synaptic-type α1β2γ2L GABAPhysiological reports · 2019Article
- Steady-State Activation and Modulation of the ConcatemericMolecular pharmacology · 2019Article
- Monod-Wyman-Changeux Allosteric Shift Analysis in MutantMolecular pharmacology · 2019Article
- Application of the Co-Agonist Concerted Transition Model to Analysis of GABAA Receptor Properties.Current neuropharmacology · 2019Review
- Analysis of GABAMolecular pharmacology · 2019Article
- Enhanced GABAergic actions resulting from the coapplication of the steroid 3α-hydroxy-5α-pregnane-11,20-dione (alfaxalone) with propofol or diazepam.Scientific reports · 2018Article
- Propofol Is an Allosteric Agonist with Multiple Binding Sites on Concatemeric Ternary GABAMolecular pharmacology · 2018Article
- GABA Type A Receptor Activation in the Allosteric Coagonist Model Framework: Relationship between ECMolecular pharmacology · 2018Article
- Article
- Mutational Analysis of the Putative High-Affinity Propofol Binding Site in Human β3 Homomeric GABAA Receptors.Molecular pharmacology · 2015Article
- Mutations at beta N265 in γ-aminobutyric acid type A receptors alter both binding affinity and efficacy of potent anesthetics.PloS one · 2014Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Etomidate is a hydrophobic molecule, a potent general anesthetic, and the best understood drug in this group. Etomidate's target molecules are GABA(A) receptors, its site of action has been identified with photolabeling, and a quantitative allosteric coagonist model has emerged for etomidate effects on GABA(A) receptors. We have shown that when methionine residues that are thought to be adjacent to the etomidate site are mutated to tryptophan, that the bulky hydrophobic side-chains alter mutant GABA(A) receptor function in ways that mimic the effects of etomidate binding to wild-type receptors. Furthermore, these mutations reduce receptor modulation by etomidate. Both of these observations support the hypothesis that these methionine residues form part of the etomidate binding pocket.
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Registered trials
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.