Tryptophan mutations at azi-etomidate photo-incorporation sites on alpha1 or beta2 subunits enhance GABAA receptor gating and reduce etomidate modulation.
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Mutations at beta N265 in γ-aminobutyric acid type A receptors alter both binding affinity and efficacy of potent anestheticsCorrection for Inhibition Leads to an Allosteric Co-Agonist Model for Pentobarbital Modulation and Activation of α1β3γ2L GABAA ReceptorsGamma-amino butyric acid type A receptor mutations at beta2N265 alter etomidate efficacy while preserving basal and agonist-dependent activityThe Molecular Mechanisms of Anesthetic Action: Updates and Cutting Edge Developments from the Field of Molecular Modeling.Numerous classes of general anesthetics inhibit etomidate binding to gamma-aminobutyric acid type A (GABAA) receptors.A residue in loop 9 of the beta2-subunit stabilizes the closed state of the GABAA receptor.Barbiturates require the N terminus and first transmembrane domain of the delta subunit for enhancement of alpha1beta3delta GABAA receptor currentsMolecular approaches to improving general anestheticsModeling anesthetic binding sites within the glycine alpha one receptor based on prokaryotic ion channel templates: the problem with TM4.Multiple Non-Equivalent Interfaces Mediate Direct Activation of GABAA Receptors by Propofol.Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular MechanismA Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude)Potentiating action of propofol at GABAA receptors of retinal bipolar cellsThe neurosteroid 5β-pregnan-3α-ol-20-one enhances actions of etomidate as a positive allosteric modulator of α1β2γ2L GABAA receptorsClinical and molecular pharmacology of etomidate.Anesthetic sites and allosteric mechanisms of action on Cys-loop ligand-gated ion channels.p-Trifluoromethyldiazirinyl-etomidate: a potent photoreactive general anesthetic derivative of etomidate that is selective for ligand-gated cationic ion channels.A Single phenylalanine residue in the main intracellular loop of α1 γ-aminobutyric acid type A and glycine receptors influences their sensitivity to propofol.An allosteric coagonist model for propofol effects on α1β2γ2L γ-aminobutyric acid type A receptors.The Direct Actions of GABA, 2'-Methoxy-6-Methylflavone and General Anaesthetics at β3γ2L GABAA Receptors: Evidence for Receptors with Different Subunit Stoichiometries.Flavan-3-ol esters: new agents for exploring modulatory sites on GABA(A) receptors.Mutations in the GABAA receptor that mimic the allosteric ligand etomidate.Two etomidate sites in α1β2γ2 γ-aminobutyric acid type A receptors contribute equally and noncooperatively to modulation of channel gating.Mutational Analysis of the Putative High-Affinity Propofol Binding Site in Human β3 Homomeric GABAA Receptors.A Cysteine Substitution Probes β3H267 Interactions with Propofol and Other Potent Anesthetics in α1β3γ2L γ-Aminobutyric Acid Type A Receptorsp-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol.State-dependent etomidate occupancy of its allosteric agonist sites measured in a cysteine-substituted GABAA receptor.Inter- and Intra-Subunit Butanol/Isoflurane Sites of Action in the Human Glycine Receptor.Allyl m-trifluoromethyldiazirine mephobarbital: an unusually potent enantioselective and photoreactive barbiturate general anesthetic.Identification of the putative binding pocket of valerenic acid on GABAA receptors using docking studies and site-directed mutagenesis.Cysteine substitutions define etomidate binding and gating linkages in the α-M1 domain of γ-aminobutyric acid type A (GABAA) receptorsThe benzodiazepine diazepam potentiates responses of α1β2γ2L γ-aminobutyric acid type A receptors activated by either γ-aminobutyric acid or allosteric agonists.GABA(A) receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation.Monod-Wyman-Changeux allosteric mechanisms of action and the pharmacology of etomidate.Mapping General Anesthetic Sites in Heteromeric γ-Aminobutyric Acid Type A Receptors Reveals a Potential For Targeting Receptor Subtypes.Mechanism of Allosteric Modulation of the Cys-loop Receptors.From the Cover: Functional Analysis Reveals Glutamate and Gamma-Aminobutyric Acid-Gated Chloride Channels as Targets of Avermectins in the Carmine Spider Mite.Neurosteroids allosterically modulate binding of the anesthetic etomidate to gamma-aminobutyric acid type A receptors.Longrange PCR-based next-generation sequencing in pharmacokinetics and pharmacodynamics study of propofol among patients under general anaesthesia.Tryptophan and Cysteine Mutations in M1 Helices of α1β3γ2L γ-Aminobutyric Acid Type A Receptors Indicate Distinct Intersubunit Sites for Four Intravenous Anesthetics and One Orphan Site.
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P2860
Tryptophan mutations at azi-etomidate photo-incorporation sites on alpha1 or beta2 subunits enhance GABAA receptor gating and reduce etomidate modulation.
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article científic
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article scientifique
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articolo scientifico
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artigo científico
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bilimsel makale
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scientific article published on 19 September 2008
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vedecký článok
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vetenskaplig artikel
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videnskabelig artikel
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vědecký článek
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name
Tryptophan mutations at azi-et ...... d reduce etomidate modulation.
@en
Tryptophan mutations at azi-et ...... d reduce etomidate modulation.
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type
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Tryptophan mutations at azi-et ...... d reduce etomidate modulation.
@en
Tryptophan mutations at azi-et ...... d reduce etomidate modulation.
@nl
prefLabel
Tryptophan mutations at azi-et ...... d reduce etomidate modulation.
@en
Tryptophan mutations at azi-et ...... d reduce etomidate modulation.
@nl
P2093
P2860
P356
P1476
Tryptophan mutations at azi-et ...... d reduce etomidate modulation.
@en
P2093
Aiping Liu
Deirdre Stewart
Rooma Desai
Stuart A Forman
P2860
P304
P356
10.1124/MOL.108.050500
P577
2008-09-19T00:00:00Z