Mutation at the putative GABA(A) ion-channel gate reveals changes in allosteric modulation.

PubWeight™: 1.01‹?› | Rank: Top 15%

🔗 View Article (PMC 1760662)

Published in Br J Pharmacol on July 01, 1999

Authors

S A Thompson1, M Z Smith, P B Wingrove, P J Whiting, K A Wafford

Author Affiliations

1: Merck Sharp & Dohme Research Laboratories, Harlow, Essex.

Articles citing this

International Union of Pharmacology. LXX. Subtypes of gamma-aminobutyric acid(A) receptors: classification on the basis of subunit composition, pharmacology, and function. Update. Pharmacol Rev (2008) 4.49

The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels. Br J Pharmacol (2013) 1.88

Methionine 286 in transmembrane domain 3 of the GABAA receptor beta subunit controls a binding cavity for propofol and other alkylphenol general anesthetics. Neuropharmacology (2001) 1.51

Tryptophan scanning mutagenesis in TM2 of the GABA(A) receptor alpha subunit: effects on channel gating and regulation by ethanol. Br J Pharmacol (2000) 1.07

Microscopic kinetic determinants of macroscopic currents: insights from coupling and uncoupling of GABAA receptor desensitization and deactivation. J Physiol (2007) 1.04

Different residues in the GABAA receptor benzodiazepine binding pocket mediate benzodiazepine efficacy and binding. Mol Pharmacol (2011) 1.00

Allosteric modulators induce distinct movements at the GABA-binding site interface of the GABA-A receptor. Neuropharmacology (2010) 0.90

Mutations of L293 in transmembrane two of the mouse 5-hydroxytryptamine3A receptor alter gating and alcohol modulatory actions. Br J Pharmacol (2006) 0.88

Allosteric modulators affect the efficacy of partial agonists for recombinant GABA(A) receptors. Br J Pharmacol (2000) 0.84

Evidence for the formation of functionally distinct alphabetagammaepsilon GABA(A) receptors. J Physiol (2001) 0.84

An engineered glutamate-gated chloride (GluCl) channel for sensitive, consistent neuronal silencing by ivermectin. J Biol Chem (2013) 0.82

The atypical cation-conduction and gating properties of ELIC underscore the marked functional versatility of the pentameric ligand-gated ion-channel fold. J Gen Physiol (2015) 0.81

Desformylflustrabromine Modulates α4β2 Neuronal Nicotinic Acetylcholine Receptor High- and Low-Sensitivity Isoforms at Allosteric Clefts Containing the β2 Subunit. J Pharmacol Exp Ther (2015) 0.80

Mapping convulsants' binding to the GABA-A receptor chloride ionophore: a proposed model for channel binding sites. Neurochem Int (2006) 0.79

Context dependent benzodiazepine modulation of GABA(A) receptor opening frequency. Curr Neuropharmacol (2010) 0.79

A spontaneous tonic chloride conductance in solitary glutamatergic hippocampal neurons. Brain Res (2006) 0.78

Articles cited by this

Acetylcholine receptor channel imaged in the open state. Nature (1995) 5.27

Which GABAA-receptor subtypes really occur in the brain? Trends Neurosci (1996) 5.18

Structure and pharmacology of gamma-aminobutyric acidA receptor subtypes. Pharmacol Rev (1995) 3.94

Mutations in the channel domain alter desensitization of a neuronal nicotinic receptor. Nature (1991) 3.52

GABAA receptor needs two homologous domains of the beta-subunit for activation by GABA but not by pentobarbital. Nature (1993) 3.49

Identification of acetylcholine receptor channel-lining residues in the entire M2 segment of the alpha subunit. Neuron (1994) 3.44

Channel gating governed symmetrically by conserved leucine residues in the M2 domain of nicotinic receptors. Nature (1995) 3.06

The role of conserved leucines in the M2 domain of the acetylcholine receptor in channel gating. Mol Pharmacol (1995) 2.45

The benzodiazepine binding site of GABAA receptors. Trends Pharmacol Sci (1997) 2.26

Stoichiometry of a recombinant GABAA receptor. J Neurosci (1996) 2.23

Identification of channel-lining residues in the M2 membrane-spanning segment of the GABA(A) receptor alpha1 subunit. J Gen Physiol (1996) 1.85

Unconventional pharmacology of a neuronal nicotinic receptor mutated in the channel domain. Proc Natl Acad Sci U S A (1992) 1.84

Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J Neurosci (1997) 1.78

Barbiturate interactions at the human GABAA receptor: dependence on receptor subunit combination. Br J Pharmacol (1996) 1.65

Single amino acid substitution affects desensitization of the 5-hydroxytryptamine type 3 receptor expressed in Xenopus oocytes. Proc Natl Acad Sci U S A (1993) 1.41

A novel allosteric modulatory site on the GABAA receptor beta subunit. Neuron (1994) 1.41

Neuronally restricted RNA splicing regulates the expression of a novel GABAA receptor subunit conferring atypical functional properties [corrected; erratum to be published]. J Neurosci (1997) 1.38

The interaction of general anaesthetics with recombinant GABAA and glycine receptors expressed in Xenopus laevis oocytes: a comparative study. Br J Pharmacol (1997) 1.37

Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human gamma-aminobutyric acid type A receptors. Mol Pharmacol (1997) 1.30

Substitutions of the highly conserved M2 leucine create spontaneously opening rho1 gamma-aminobutyric acid receptors. Mol Pharmacol (1998) 1.26

Homomeric beta 1 gamma-aminobutyric acid A receptor-ion channels: evaluation of pharmacological and physiological properties. Mol Pharmacol (1996) 1.18

Key amino acids in the gamma subunit of the gamma-aminobutyric acidA receptor that determine ligand binding and modulation at the benzodiazepine site. Mol Pharmacol (1997) 1.02

The rat beta 1-subunit of the GABAA receptor forms a picrotoxin-sensitive anion channel open in the absence of GABA. FEBS Lett (1989) 0.97

Effects of mutating leucine to threonine in the M2 segment of alpha1 and beta1 subunits of GABAA alpha1beta1 receptors. J Membr Biol (1996) 0.95

Agonist-induced closure of constitutively open gamma-aminobutyric acid channels with mutated M2 domains. Proc Natl Acad Sci U S A (1997) 0.93

Articles by these authors

Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype. Nat Neurosci (2000) 5.53

Which GABAA-receptor subtypes really occur in the brain? Trends Neurosci (1996) 5.18

Pharmacological characterization of a novel cell line expressing human alpha(4)beta(3)delta GABA(A) receptors. Br J Pharmacol (2002) 3.38

Disrupted in Schizophrenia 1 Interactome: evidence for the close connectivity of risk genes and a potential synaptic basis for schizophrenia. Mol Psychiatry (2006) 3.33

The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid. Proc Natl Acad Sci U S A (1997) 2.73

Cerebrovascular disease and threshold for dementia in the early stages of Alzheimer's disease. Lancet (1999) 2.11

Preferential coassembly of alpha4 and delta subunits of the gamma-aminobutyric acidA receptor in rat thalamus. Mol Pharmacol (1999) 1.96

Functional characterization of human gamma-aminobutyric acidA receptors containing the alpha 4 subunit. Mol Pharmacol (1996) 1.88

Molecular and functional diversity of the expanding GABA-A receptor gene family. Ann N Y Acad Sci (1999) 1.71

Growth factors regulate the survival and fate of cells derived from human neurospheres. Nat Biotechnol (2001) 1.70

Nicotine-induced increase in neuronal nicotinic receptors results from a decrease in the rate of receptor turnover. Mol Pharmacol (1994) 1.68

Barbiturate interactions at the human GABAA receptor: dependence on receptor subunit combination. Br J Pharmacol (1996) 1.65

Disrupted in Schizophrenia 1 and Nudel form a neurodevelopmentally regulated protein complex: implications for schizophrenia and other major neurological disorders. Mol Cell Neurosci (2004) 1.62

Pharmacological properties of recombinant human N-methyl-D-aspartate receptors comprising NR1a/NR2A and NR1a/NR2B subunit assemblies expressed in permanently transfected mouse fibroblast cells. Mol Pharmacol (1995) 1.58

Molecular pharmacology of gamma-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different alpha, beta, and gamma receptor subunit combinations. Mol Pharmacol (1994) 1.57

theta, a novel gamma-aminobutyric acid type A receptor subunit. Proc Natl Acad Sci U S A (1999) 1.54

The Cys-loop superfamily of ligand-gated ion channels: the impact of receptor structure on function. Biochem Soc Trans (2004) 1.53

Expression of disrupted in schizophrenia 1 (DISC1) protein in the adult and developing mouse brain indicates its role in neurodevelopment. Mol Psychiatry (2004) 1.51

alpha4beta3delta GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J Biol Chem (2001) 1.48

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. Proc Natl Acad Sci U S A (1994) 1.48

Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. Mol Pharmacol (1993) 1.44

Structure and pharmacology of vertebrate GABAA receptor subtypes. Int Rev Neurobiol (1995) 1.42

A novel allosteric modulatory site on the GABAA receptor beta subunit. Neuron (1994) 1.41

Stoichiometry of a ligand-gated ion channel determined by fluorescence energy transfer. J Biol Chem (1999) 1.41

Neuronally restricted RNA splicing regulates the expression of a novel GABAA receptor subunit conferring atypical functional properties [corrected; erratum to be published]. J Neurosci (1997) 1.38

Loss of the major GABA(A) receptor subtype in the brain is not lethal in mice. J Neurosci (2001) 1.37

Role of the beta subunit in determining the pharmacology of human gamma-aminobutyric acid type A receptors. Mol Pharmacol (1993) 1.34

Assembly intracellular targeting and cell surface expression of the human N-methyl-D-aspartate receptor subunits NR1a and NR2A in transfected cells. Neuropharmacology (1999) 1.31

Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human gamma-aminobutyric acid type A receptors. Mol Pharmacol (1997) 1.30

An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition. J Pharmacol Exp Ther (2005) 1.28

Anticonvulsant and adverse effects of avermectin analogs in mice are mediated through the gamma-aminobutyric acid(A) receptor. J Pharmacol Exp Ther (2000) 1.26

Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux. Mol Pharmacol (2001) 1.26

Anaesthetic concentrations of alcohols potentiate GABAA receptor-mediated currents: lack of subunit specificity. Eur J Pharmacol (1994) 1.22

Differences in affinity and efficacy of benzodiazepine receptor ligands at recombinant gamma-aminobutyric acidA receptor subtypes. Mol Pharmacol (1993) 1.21

Genetic knockout and pharmacological blockade studies of the 5-HT7 receptor suggest therapeutic potential in depression. Neuropharmacology (2005) 1.18

Immunohistochemical localization of neuronal nicotinic receptors in the rodent central nervous system. J Neurosci (1987) 1.14

Ethanol potentiation of GABAA receptors requires phosphorylation of the alternatively spliced variant of the gamma 2 subunit. FEBS Lett (1992) 1.12

Functional comparison of the role of gamma subunits in recombinant human gamma-aminobutyric acidA/benzodiazepine receptors. Mol Pharmacol (1993) 1.10

Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol (1996) 1.09

Salicylidene salicylhydrazide, a selective inhibitor of beta 1-containing GABAA receptors. Br J Pharmacol (2004) 1.05

beta-Carboline gamma-aminobutyric acidA receptor inverse agonists modulate gamma-aminobutyric acid via the loreclezole binding site as well as the benzodiazepine site. Mol Pharmacol (1995) 1.04

Preferential co-assembly of recombinant NMDA receptors composed of three different subunits. Neuroreport (1993) 1.04

A single amino acid of the human gamma-aminobutyric acid type A receptor gamma 2 subunit determines benzodiazepine efficacy. J Biol Chem (1994) 1.03

Key amino acids in the gamma subunit of the gamma-aminobutyric acidA receptor that determine ligand binding and modulation at the benzodiazepine site. Mol Pharmacol (1997) 1.02

Subcellular targeting of DISC1 is dependent on a domain independent from the Nudel binding site. Mol Cell Neurosci (2005) 1.01

Model of subunit composition of gamma-aminobutyric acid A receptor subtypes expressed in rat cerebellum with respect to their alpha and gamma/delta subunits. J Biol Chem (1994) 1.01

Identification of amino acids in the N-methyl-D-aspartate receptor NR1 subunit that contribute to the glycine binding site. Mol Pharmacol (1995) 1.00

Actions of the general anesthetic propofol on recombinant human GABAA receptors: influence of receptor subunits. J Pharmacol Exp Ther (1995) 1.00

Functional acetylcholine receptor in PC12 cells reacts with a monoclonal antibody to brain nicotinic receptors. Nature (1987) 1.00

MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. J Psychopharmacol (2010) 0.99

Ethanol, flunitrazepam, and pentobarbital modulation of GABAA receptors expressed in mammalian cells and Xenopus oocytes. Alcohol Clin Exp Res (1997) 0.99

Purification and characterization of a nicotinic acetylcholine receptor from chick brain. Biochemistry (1986) 0.98

Special relationship of gamma-aminobutyric acid to the ventromedial nucleus of the hypothalamus during embryonic development. J Comp Neurol (1999) 0.98

GABA receptors on the cell-body membrane of an identified insect motor neuron. Proc R Soc Lond B Biol Sci (1988) 0.98

Alpha subunit isoform influences GABA(A) receptor modulation by propofol. Neuropharmacology (1997) 0.97

Differential effects of NMDA antagonists on high frequency and gamma EEG oscillations in a neurodevelopmental model of schizophrenia. Neuropharmacology (2011) 0.97

Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist. J Psychopharmacol (2010) 0.97

Antibody heterogeneity and specificity in myasthenia gravis. Ann N Y Acad Sci (1987) 0.96

Characterisation of delta-subunit containing GABAA receptors from rat brain. Eur J Pharmacol (1995) 0.96

Stable expression of mammalian type A gamma-aminobutyric acid receptors in mouse cells: demonstration of functional assembly of benzodiazepine-responsive sites. Proc Natl Acad Sci U S A (1992) 0.96

A study of subunit selectivity, mechanism and site of action of the delta selective compound 2 (DS2) at human recombinant and rodent native GABA(A) receptors. Br J Pharmacol (2013) 0.94

Identification of amino acid residues responsible for the alpha5 subunit binding selectivity of L-655,708, a benzodiazepine binding site ligand at the GABA(A) receptor. J Neurochem (2001) 0.94

Cloning, functional coexpression, and pharmacological characterisation of human cDNAs encoding NMDA receptor NR1 and NR2A subunits. J Neurochem (1994) 0.94

Platelet-derived growth factor induces a long-term inhibition of N-methyl-D-aspartate receptor function. J Biol Chem (1996) 0.93

Myasthenia gravis: monoclonal antihuman acetylcholine receptor antibodies used to analyze antibody specificities and responses to treatment. Neurology (1986) 0.91

Residues in transmembrane domains I and II determine gamma-aminobutyric acid type AA receptor subtype-selective antagonism by furosemide. Mol Pharmacol (1999) 0.91

Overexpression of the GABA(A) receptor epsilon subunit results in insensitivity to anaesthetics. Neuropharmacology (2002) 0.90

The non-peptidyl fungal metabolite L-783,281 activates TRK neurotrophin receptors. J Neurochem (2001) 0.90

Acetylcholine receptor antibody characteristics in myasthenia gravis. Fractionation of alpha-bungarotoxin binding site antibodies and their relationship to IgG subclass. J Neuroimmunol (1983) 0.89

Monoclonal antibodies that distinguish between normal and denervated human acetylcholine receptor. J Neuroimmunol (1986) 0.89

Cell surface expression of the human N-methyl-D-aspartate receptor subunit 1a requires the co-expression of the NR2A subunit in transfected cells. Neuroscience (1996) 0.88

Recombinant human NMDA homomeric NR1 receptors expressed in mammalian cells form a high-affinity glycine antagonist binding site. J Neurochem (1995) 0.86

Effects of 5-HT3 receptor antagonists on binding and function of mouse and human GABAA receptors. Eur J Pharmacol (1994) 0.86

Ethanol increases GABAA responses in cells stably transfected with receptor subunits. Alcohol Clin Exp Res (1995) 0.86

The pharmacology of the benzodiazepine site of the GABA-A receptor is dependent on the type of gamma-subunit present. J Recept Signal Transduct Res (1997) 0.85

Agonist activation and alpha-bungarotoxin inhibition of wild type and mutant alpha7 nicotinic acetylcholine receptors. Eur J Pharmacol (1999) 0.85

Allosteric modulators affect the efficacy of partial agonists for recombinant GABA(A) receptors. Br J Pharmacol (2000) 0.84

Microtubule depolymerization inhibits ethanol-induced enhancement of GABAA responses in stably transfected cells. J Neurochem (1996) 0.84

Effects of amino acid neurotransmitter candidates on an identified insect motoneurone. Neurosci Lett (1986) 0.84