Functional sites involved in modulation of the GABAA receptor channel by the intravenous anesthetics propofol, etomidate and pentobarbital

[1]  E. Sigel,et al.  Positive modulation of synaptic and extrasynaptic GABAA receptors by an antagonist of the high affinity benzodiazepine binding site , 2015, Neuropharmacology.

[2]  D. C. Chiara,et al.  Positive and Negative Allosteric Modulation of an α1β3γ2 γ-Aminobutyric Acid Type A (GABAA) Receptor by Binding to a Site in the Transmembrane Domain at the γ+-β− Interface* , 2015, The Journal of Biological Chemistry.

[3]  S. Forman,et al.  Mutations at Beta N265 in γ-Aminobutyric Acid Type A Receptors Alter Both Binding Affinity and Efficacy of Potent Anesthetics , 2014, PloS one.

[4]  R. Eckenhoff,et al.  Multiple Propofol-binding Sites in a γ-Aminobutyric Acid Type A Receptor (GABAAR) Identified Using a Photoreactive Propofol Analog*♦ , 2014, The Journal of Biological Chemistry.

[5]  Erwin Sigel,et al.  Accelerated discovery of novel benzodiazepine ligands by experiment-guided virtual screening. , 2014, ACS chemical biology.

[6]  Edward H. Smith,et al.  A propofol binding site on mammalian GABAA receptors identified by photolabeling , 2013, Nature chemical biology.

[7]  D. C. Chiara,et al.  Specificity of Intersubunit General Anesthetic-binding Sites in the Transmembrane Domain of the Human α1β3γ2 γ-Aminobutyric Acid Type A (GABAA) Receptor*♦ , 2013, The Journal of Biological Chemistry.

[8]  E. Sigel,et al.  Structure, Function, and Modulation of GABAA Receptors* , 2012, The Journal of Biological Chemistry.

[9]  S. Forman,et al.  Two Etomidate Sites in &agr;1&bgr;2&ggr;2 &ggr;-Aminobutyric Acid Type A Receptors Contribute Equally and Noncooperatively to Modulation of Channel Gating , 2012, Anesthesiology.

[10]  J. Hanrahan,et al.  Flavan‐3‐ol esters: new agents for exploring modulatory sites on GABAA receptors , 2012, British journal of pharmacology.

[11]  D. C. Chiara,et al.  Mapping general anesthetic binding site(s) in human α1β3 γ-aminobutyric acid type A receptors with [³H]TDBzl-etomidate, a photoreactive etomidate analogue. , 2012, Biochemistry.

[12]  Eric Gouaux,et al.  Principles of activation and permeation in an anion-selective Cys-loop receptor , 2011, Nature.

[13]  J. Trudell,et al.  A Transmembrane Amino Acid in the GABAA Receptor β2 Subunit Critical for the Actions of Alcohols and Anesthetics , 2010, Journal of Pharmacology and Experimental Therapeutics.

[14]  T. Smart,et al.  Binding, activation and modulation of Cys-loop receptors. , 2010, Trends in pharmacological sciences.

[15]  R. Olsen,et al.  Numerous Classes of General Anesthetics Inhibit Etomidate Binding to γ-Aminobutyric Acid Type A (GABAA) Receptors* , 2010, The Journal of Biological Chemistry.

[16]  R. Olsen,et al.  Neurosteroids Allosterically Modulate Binding of the Anesthetic Etomidate to γ-Aminobutyric Acid Type A Receptors* , 2009, Journal of Biological Chemistry.

[17]  Werner Sieghart,et al.  International Union of Pharmacology. LXX. Subtypes of γ-Aminobutyric AcidA Receptors: Classification on the Basis of Subunit Composition, Pharmacology, and Function. Update , 2008, Pharmacological Reviews.

[18]  A. Jenkins,et al.  A Conserved Tyrosine in the β2 Subunit M4 Segment Is a Determinant of γ-Aminobutyric Acid Type A Receptor Sensitivity to Propofol , 2007 .

[19]  M. Arras,et al.  Identification of a Molecular Target Mediating the General Anesthetic Actions of Pentobarbital , 2007, Molecular Pharmacology.

[20]  R. Olsen,et al.  Identification of a GABAA Receptor Anesthetic Binding Site at Subunit Interfaces by Photolabeling with an Etomidate Analog , 2006, The Journal of Neuroscience.

[21]  E. Sigel,et al.  A GABAA receptor of defined subunit composition and positioning: Concatenation of five subunits , 2006, FEBS letters.

[22]  E. Sigel,et al.  Consequence of the presence of two different β subunit isoforms in a GABAA receptor , 2005 .

[23]  W. Ernst.  Heterogeneity of GABAA Receptors: Revived Interest in the Development of Subtype-selective Drugs , 2005 .

[24]  J. Lambert,et al.  Neurosteroids: endogenous regulators of the GABAA receptor , 2005, Nature Reviews Neuroscience.

[25]  M. Farrant,et al.  Variations on an inhibitory theme: phasic and tonic activation of GABAA receptors , 2005, Nature Reviews Neuroscience.

[26]  E. Sigel,et al.  The Xenopus oocyte: system for the study of functional expression and modulation of proteins. , 2005, Molecular nutrition & food research.

[27]  E. Sigel,et al.  Positioning of the α-subunit isoforms confers a functional signature to γ-aminobutyric acid type A receptors , 2004 .

[28]  E. Sigel,et al.  Individual Properties of the Two Functional Agonist Sites in GABAA Receptors , 2003, The Journal of Neuroscience.

[29]  U. Rudolph,et al.  Mutational analysis of molecular requirements for the actions of general anaesthetics at the γ-aminobutyric acidA receptor subtype, α1β2γ2 , 2003, BMC pharmacology.

[30]  B. Antkowiak,et al.  General anesthetic actions in vivo strongly attenuated by a point mutation in the GABAA receptor β3 subunit , 2003, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[31]  Erwin Sigel,et al.  Forced subunit assembly in α1β2γ2 GABAA receptors: insight into the absolute arrangement , 2002 .

[32]  E. Sigel,et al.  The relative amount of cRNA coding for γ2 subunits affects stimulation by benzodiazepines in GABAA receptors expressed in Xenopus oocytes , 2002, Neuropharmacology.

[33]  A. Jenkins,et al.  Volatile anesthetic actions on the GABAA receptors: contrasting effects of α1(S270) and β2(N265) point mutations , 2002, Neuropharmacology.

[34]  U. Rudolph,et al.  Molecular determinants for the action of general anesthetics 
at recombinant α2β3γ2γ‐aminobutyric acidA receptors , 2002, Journal of neurochemistry.

[35]  E. Sigel,et al.  Subunit Arrangement of γ-Aminobutyric Acid Type A Receptors* , 2001, The Journal of Biological Chemistry.

[36]  S. Forman,et al.  The γ Subunit Determines Whether Anesthetic-induced Leftward Shift Is Altered by a Mutation at α1S270 in α1β2γ2L GABAA Receptors , 2001 .

[37]  J. Amin,et al.  Benzodiazepines act on GABAA receptors via two distinct and separable mechanisms , 2000, Nature Neuroscience.

[38]  R. Mckernan,et al.  Stoichiometry of a Ligand-gated Ion Channel Determined by Fluorescence Energy Transfer* , 1999, The Journal of Biological Chemistry.

[39]  G. Biggio,et al.  International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function. , 1998, Pharmacological reviews.

[40]  E. Sigel,et al.  The benzodiazepine binding site of GABAA receptors. , 1997, Trends in pharmacological sciences.

[41]  P. Whiting,et al.  The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid. , 1997, Proceedings of the National Academy of Sciences of the United States of America.

[42]  E. Sigel,et al.  ReviewThe benzodiazepine binding site of GABAA receptors , 1997 .

[43]  Werner Sieghart,et al.  Stoichiometry and Assembly of a Recombinant GABAA Receptor Subtype , 1997, The Journal of Neuroscience.

[44]  D. S. Weiss,et al.  Stoichiometry of a Recombinant GABAA Receptor , 1996, The Journal of Neuroscience.

[45]  S. Russek,et al.  From ion currents to genomic analysis: Recent advances in GABAA receptor research , 1995, Synapse.

[46]  W. Sieghart,et al.  Structure and pharmacology of gamma-aminobutyric acidA receptor subtypes. , 1995, Pharmacological reviews.

[47]  P. Whiting,et al.  The modulatory action of loreclezole at the gamma-aminobutyric acid type A receptor is determined by a single amino acid in the beta 2 and beta 3 subunit. , 1994, Proceedings of the National Academy of Sciences of the United States of America.

[48]  Gerhard Trube,et al.  The effect of subunit composition of rat brain GABAA receptors on channel function , 1990, Neuron.

[49]  H. Betz.  Ligand-gated ion channels in the brain: The amino acid receptor superfamily , 1990, Neuron.

[50]  E. Sigel.  Properties of single sodium channels translated by Xenopus oocytes after injection with messenger ribonucleic acid. , 1987, The Journal of physiology.

[51]  E. Sigel,et al.  A closer look at the high affinity benzodiazepine binding site on GABAA receptors. , 2011, Current topics in medicinal chemistry.

[52]  M. Akabas,et al.  Defining the propofol binding site location on the GABAA receptor. , 2004, Molecular pharmacology.

[53]  R. Olsen,et al.  GABAA receptor channels. , 1994, Annual review of neuroscience.