GABAA receptor pharmacology
Data up to Jan 2025
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Abstract
References (337)
Steroid Hormone Metabolites Are Barbiturate-Like Modulators of the GABA Receptor
1986 • 2,194 citations
GABAA Receptor Channels
1994 • 1,948 citations
Sequence and functional expression of the GABAA receptor shows a ligand-gated receptor super-family
1987 • 1,621 citations
Benzodiazepine receptors in rat brain
1977 • 1,459 citations
Importance of a novel GABAA receptor subunit for benzodiazepine pharmacology
1989 • 1,283 citations
Amino acid transmitters in the mammalian central nervous system
1974 • 1,169 citations
Mechanism of anion permeation through channels gated by glycine and gamma‐aminobutyric acid in mouse cultured spinal neurones.
1987 • 1,166 citations
Phospholipid Methylation and Biological Signal Transmission
1980 • 1,101 citations
3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABAB sites in rat brain
1981 • 1,044 citations
Stress-induced elevations of gamma-aminobutyric acid type A receptor-active steroids in the rat brain.
1991 • 943 citations
A Review of Psychoendocrine Research on the Pituitary-Adrenal Cortical System
1968 • 874 citations
Pharmacological studies on presynaptic inhibition
1963 • 765 citations
GABAergic modulation of benzodiazepine binding site sensitivity
1978 • 726 citations
Bicuculline, an antagonist of GABA and synaptic inhibition in the spinal cord of the cat
1971 • 685 citations
Ionic basis of GABAA receptor channel function in the nervous system
1994 • 679 citations
Interaction of Convulsive Ligands with Benzodiazepine Receptors
1982 • 549 citations
GABA, Bicuculline and Central Inhibition
1970 • 545 citations
Quantal analysis of inhibitory synaptic transmission in the dentate gyrus of rat hippocampal slices: a patch‐clamp study.
1990 • 545 citations
Evolutionary history of the ligand-gated ion-channel superfamily of receptors
1995 • 535 citations
Modulation of the GABA receptor complex by a steroid anaesthetic
1984 • 496 citations
Modulation of the N-methyl-D-aspartate channel by extracellular H+.
1990 • 458 citations
Potentiation of NMDA receptor currents by arachidonic acid
1992 • 428 citations
Quaternary Structure of the Native GABAA Receptor Determined by Electron Microscopic Image Analysis
1994 • 423 citations
GABAA receptor needs two homologous domains of the & beta;-subunit for activation by GABA but not by pentobarbital
1993 • 417 citations
Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor
1995 • 408 citations
Neurosteroid biosynthesis: genes for adrenal steroidogenic enzymes are expressed in the brain
1993 • 402 citations
GABAA receptors: ligand-gated Cl− ion channels modulated by multiple drug-binding sites
1992 • 382 citations
CORRELATIONS BETWEEN THE CHEMICAL STRUCTURE AND THE PHARMACOLOGICAL ACTIONS OF THE STEROIDS1
1942 • 348 citations
A new class of GABA agonist
1977 • 338 citations
Influence of recombinant gamma-aminobutyric acid-A receptor subunit composition on the action of allosteric modulators of gamma-aminobutyric acid-gated Cl- currents.
1991 • 338 citations
INHIBITION OF GABA UPTAKE IN RAT BRAIN SLICES BY NIPECOTIC ACID, VARIOUS ISOXAZOLES AND RELATED COMPOUNDS
1975 • 329 citations
Functional Modulation of GABA A Receptors by cAMP-Dependent Protein Phosphorylation
1992 • 322 citations
Physiological evidence for two distinct GABAA responses in rat hippocampus
1993 • 304 citations
Neurosteroids: a new function in the brain
1991 • 296 citations
Zolpidem
1990 • 290 citations
STRUCTURE AND BIOLOGICAL ACTIVITY OF A SERIES OF CONFORMATIONALLY RESTRICTED ANALOGUES OF GABA
1975 • 267 citations
The inhibitory action of noradrenaline and other monoamines on spinal neurones
1966 • 262 citations
Neurosteroid regulation of GABAA receptor single‐channel kinetic properties of mouse spinal cord neurons in culture.
1992 • 241 citations
Diazepam-Binding Inhibitor: A Neuropeptide Located in Selected Neuronal Populations of Rat Brain
1985 • 228 citations
Pregnenolone sulfate potentiation of N-methyl-D-aspartate receptor channels in hippocampal neurons.
1993 • 223 citations
GABAA receptors are differentially sensitive to zinc: dependence on subunit composition
1991 • 223 citations
Gaba agonists and antagonists
1979 • 222 citations
Noise analysis of miniature IPSCs in adult rat brain slices: properties and modulation of synaptic GABAA receptor channels
1994 • 222 citations
Barbiturate regulation of kinetic properties of the GABAA receptor channel of mouse spinal neurones in culture.
1989 • 216 citations
Benzodiazepine and beta‐carboline regulation of single GABAA receptor channels of mouse spinal neurones in culture.
1994 • 214 citations
Neuropharmacology of Amino Acid Inhibitory Transmitters
1978 • 212 citations
Central actions of ibotenic acid and muscimol
1968 • 208 citations
Point mutations affecting antagonist affinity and agonist dependent gating of GABAA receptor channels.
1992 • 203 citations
Chronic ethanol administration alters gamma-aminobutyric acidA receptor gene expression.
1992 • 200 citations
Neurotransmitter-gated ion channels as unconventional allosteric proteins
1994 • 197 citations
Role of the beta subunit in determining the pharmacology of human gamma-aminobutyric acid type A receptors.
1993 • 194 citations
On the mechanism of action of picrotoxin on GABA receptor channels in dissociated sympathetic neurones of the rat.
1992 • 193 citations
Chrysin (5,7-di-OH-flavone), a naturally-occurring ligand for benzodiazepine receptors, with anticonvulsant properties
1990 • 188 citations
Steroid modulation of the GABA/benzodiazepine receptor-linked chloride lonophore
1988 • 187 citations
Ethanol potentiation of GABAA receptors requires phosphorylation of the alternatively spliced variant of the γ2 subunit
1992 • 178 citations
CIS‐ AND TRANS‐4‐AMINOCROTONIC ACID AS GABA ANALOGUES OF RESTRICTED CONFORMATION
1975 • 176 citations
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.
1994 • 172 citations
Convulsive action of penicillin
1972 • 170 citations
Diazepam enhancement of low affinity GABA binding to rat brain membranes
1982 • 166 citations
Interleukin-1 augments gamma-aminobutyric acidA receptor function in brain.
1991 • 165 citations
Positive modulation of human gamma-aminobutyric acid type A and glycine receptors by the inhalation anesthetic isoflurane.
1993 • 164 citations
Stoichiometry of a recombinant GABAA receptor deduced from mutation-induced rectification
1993 • 164 citations
Glucocorticoid Physiology, Pharmacology and Stress
1986 • 159 citations
Amino acids as chemical transmitters
1979 • 158 citations
Evidence that bicuculline and picrotoxin act at separate sites to antagonize γ-aminobutyric acid in rat cuneate nucleus
1980 • 158 citations
OCCLUSION AND METABOLISM OF γ‐AMINOBUTYRIC ACID BY BRAIN TISSUE*
1958 • 157 citations
Die Wirkung von Diazepam auf die pr�synaptische Hemmung und andere R�ckenmarksreflexe
1967 • 156 citations
Electrophysiological studies on the specific benzodiazepine antagonist Ro 15-1788
1981 • 156 citations
Effects of two benzodiazepines, phenobarbitone, and baclofen on synaptic transmission in the cat cuneate nucleus
1976 • 155 citations
Emerging neurochemical concepts in the actions of ethanol at ligand-gated ion channels
1994 • 154 citations
Selective antagonist for the cerebellar granule cell-specific gamma-aminobutyric acid type A receptor.
1995 • 152 citations
Neurosteroids modulate calcium currents in hippocampal CA1 neurons via a pertussis toxin-sensitive G-protein-coupled mechanism
1994 • 147 citations
Bicuculline Methochloride as a GABA Antagonist
1972 • 145 citations
ADVERSE REACTIONS TO INTRAVENOUS ANAESTHETICS: A Survey of 100 Reports
1975 • 145 citations
Multiple mechanisms of picrotoxin block of GABA‐induced currents in rat hippocampal neurons.
1993 • 144 citations
3 alpha-Hydroxy-5 beta-pregnan-20-one sulfate: a negative modulator of the NMDA-induced current in cultured neurons.
1994 • 142 citations
Functional diversity of GABA activated Cl− currents in Purkinje versus granule neurons in rat cerebellar slices
1994 • 142 citations
Does neurosteroid modulatory efficacy depend on GABAA receptor subunit composition?
1993 • 140 citations
Gamma‐aminobutyric acid uptake and the termination of inhibitory synaptic potentials in the rat hippocampal slice.
1985 • 139 citations
General anesthetics potentiate gamma-aminobutyric acid actions on gamma-aminobutyric acidA receptors expressed by Xenopus oocytes: lack of involvement of intracellular calcium.
1992 • 139 citations
Bicuculline and picrotoxin block γ-aminobutryic acid-gated Cl− conductance by different mechanisms
1985 • 136 citations
Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site
1986 • 134 citations
Estrogen regulation of GABAA receptor subunit mRNA expression in preoptic area and bed nucleus of the stria terminalis of female rat brain
1995 • 133 citations
A novel modulatory binding site for zinc on the GABAA receptor complex in cultured rat neurones.
1992 • 132 citations
Insecticide action at the GABA‐gated chloride channel: Recognition, progress, and prospects
1993 • 131 citations
Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors.
1990 • 130 citations
Analgesic properties of the GABA-minetic thip
1981 • 130 citations
Benzodiazepine and β-adrenergic receptor ligands independently stimulate phospholipid methylation
1979 • 128 citations
Role of GABAA receptors in the actions of alcohol and in alcoholism: recent advances.
1994 • 127 citations
The function of acyl-CoA-binding protein (ACBP)/Diazepam binding inhibitor (DBI)
1993 • 125 citations
Securinine alkaloids: A new class of GABA receptor antagonist
1985 • 121 citations
Potentiation of GABAA-mediated synaptic current by ethanol in hippocampal CA1 neurons: possible role of protein kinase C.
1994 • 117 citations
Rapid changes in GABA binding induced by stress in different areas of the rat brain
1981 • 115 citations
Acute stress enhances the activity of the GABA receptor-gated chloride ion channel in brain
1987 • 113 citations
Isolation of pharmacologically active benzodiazepine receptor ligands from Tilia tomentosa (Tiliaceae)
1994 • 112 citations
Differential effect of zinc on the vertebrate GABAA‐receptor complex
1990 • 112 citations
The Role of Peptides and Amino Acids as Neurotransmitters
1982 • 111 citations
[3H]Bicuculline Methochloride Binding to Low‐Affinity γ‐Aminobutyric Acid Receptor Sites
1983 • 108 citations
Sodium and GABA-activated channels as the targets of pyrethroids and cyclodienes
1992 • 105 citations
Potentiation of GABA-mediated currents by cAMP-dependent protein kinase
1992 • 104 citations
Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogs of 6-(benzyloxy)-4-(methoxymethyl)-.beta.-carboline-3-carboxylic acid ethyl ester
1990 • 104 citations
Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of .gamma.-aminobutyric acid acting as selective GABA-A antagonists
1987 • 104 citations
Pentobarbital: Stereospecific Actions of (+) and (-) Isomers Revealed on Cultured Mammalian Neurons
1980 • 104 citations
Anticonvulsant and anesthetic barbiturates
1979 • 104 citations
Taurine and β-alanine act on both GABA and glycine receptors in Xenopus oocyte injected with mouse brain messenger RNA
1988 • 102 citations
GABAA Receptor Agonists, Partial Agonists, and Antagonists. Design and Therapeutic Prospects
1994 • 102 citations
Penicillin and inhibition in the cat spinal cord
1972 • 99 citations
Structure-activity relationships in steroidal anaesthetics
1975 • 98 citations
Properties of gamma-aminobutyric acid receptor binding with (+)-[3H]bicuculline methiodide in rat cerebellum.
1978 • 93 citations
Chemical instability of the GABA antagonist bicuculline under physiological conditions
1975 • 89 citations
A steroid derivative, R 5135, antagonizes the GABA/benzodiazepine receptor interaction
1981 • 88 citations
Effects of Ro15-4513 and other benzodiazepine receptor inverse agonists on alcohol-induced intoxication in the rat.
1988 • 87 citations
High affinity of the naturally-occurring biflavonoid, amentoflavon, to brain benzodiazepine receptors in vitro
1988 • 87 citations
Pharmacology of Barbiturates: Electrophysiological and Neurochemical Studies
1983 • 87 citations
Anaesthetic concentrations of alcohols potentiate GABAA receptor-mediated currents: lack of subunit specificity
1994 • 86 citations
Differential antagonism by epipregnanolone of alphaxalone and pregnanolone potentiation of [3H]flunitrazepam binding suggests more than one class of binding site for steroids at GABAA receptors
1993 • 85 citations
The rapidly expanding range of neuronal benzodiazepine receptor ligands
1993 • 84 citations
Steroid Modulation of the GABA A Receptor Complex: Electrophysiological Studies
2007 • 83 citations
GABA agonists and antagonists
1992 • 83 citations
GABA ρ2 receptor pharmacological profile: GABA recognition site similarities to ρ1
1993 • 83 citations
Pharmacological receptors and general permeability phenomena of cell membranes
1965 • 82 citations
Prediction of Receptor Properties and Binding Affinity of Ligands to Benzodiazepine/GABAA Receptors Using Artificial Neural Networks
1995 • 81 citations
Multiple distinct subunits of the gamma-aminobutyric acid-A receptor protein show different ligand-binding affinities.
1990 • 81 citations
Increased GABA binding in mouse brain following acute swim stress
1981 • 81 citations
Glycine, strychnine, picrotoxin and spinal inhibition
1969 • 80 citations
Ethanol differentially modulates GABAA receptor‐mediated chloride currents in hippocampal, cortical, and septal neurons in rat brain slices
1994 • 79 citations
The rat β1 ‐subunit of the GABAA receptor forms a picrotoxin‐sensitive anion channel open in the absence of GABA
1989 • 76 citations
The influence of estrus cycle on neurosteroid potency at the gamma-aminobutyric acidA receptor complex.
1993 • 76 citations
Spontaneous and GABA-evoked chloride channels on pituitary intermediate lobe cells and their internal Ca requirements
1987 • 76 citations
Brain γ-aminobutyric acid receptor binding is normal in rats with thioacetamide-induced hepatic encephalopathy despite elevated plasma γ-aminobutyric acid-like activity
1987 • 75 citations
Antagonist-type interaction of glucocorticoids with the GABA receptor-coupled chloride channel
1987 • 75 citations
γ‐AMINOBUTYRIC ACID AGONISTS: AN in vitro COMPARISON BETWEEN DEPRESSION OF SPINAL SYNAPTIC ACTIVITY AND DEPOLARIZATION OF SPINAL ROOT FIBRES IN THE RAT
1980 • 75 citations
Structure and molecular modeling of GABAA receptor antagonists
1992 • 75 citations
Current potentiation by diazepam but not GABA sensitivity is determined by a single histidine residue
1993 • 74 citations
Differential modulation of GABAA receptor-channel complex by polyvalent cations in rat dorsal root ganglion neurons
1993 • 74 citations
Antagonism of GABAA receptors by 4-quinolones
1993 • 72 citations
Presence of a low molecular weight endogenous inhibitor on 3H-muscimol binding in synaptic membranes
1980 • 71 citations
Compounds from Danshen. Part 4. Structure-activity relationship of miltirone, an active central benzodiazepine receptor ligand isolated from Salvia miltiorrhiza Bunge (Danshen)
1991 • 71 citations
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor
1994 • 71 citations
Natural mutation of GABAA receptor α6 subunit alters benzodiazepine affinity but not allosteric GABA effects
1993 • 70 citations
Some properties of 3H-diazepam displacing activity from human urine
1979 • 70 citations
Benzodiazepine receptors and diazepam binding inhibitor: A possible link between stress, anxiety and the immune system
1993 • 69 citations
α subunits influence Zn block of γ2 containing GABAA receptor currents
1995 • 66 citations
Neuropoisons: Their Pathophysiological Actions
2012 • 66 citations
Assembly of GABAA receptor subunits determines sorting and localization in polarized cells
1993 • 65 citations
Dual activation of GABAA and glycine receptors by β-alanine: inverse modulation by progesterone and 5α-pregnan-3α-ol-20-one
1993 • 65 citations
Trichloroethanol potentiates synaptic transmission mediated by gamma-aminobutyric acidA receptors in hippocampal neurons.
1993 • 64 citations
Disruption of GABA-dependent chloride flux by cyclodienes and hexachlorocyclohexanes in primary cultures of cortical neurons.
1994 • 63 citations
Synthetic analogs for the study of GABA as a neurotransmitter
1983 • 63 citations
Pitrazepin, a novel GABAA antagonist
1984 • 63 citations
The effect of phospholipases and proteases on the binding of γ-aminobutyric acid to junctional complexes of rat cerebellum
1976 • 62 citations
Miltirone, a central benzodiazepine receptor partial agonist from a Chinese medicinal herb Salvia Miltiorrhiza
1991 • 61 citations
Volatile anesthetics bidirectionally and stereospecifically modulate ligand binding to GABA receptors
1994 • 61 citations
Differential pharmacological effects of benzodiazepine receptor inverse agonists.
1983 • 61 citations
The analgesic effect of the GABA‐agonist THIP in patients with chronic pain of malignant origin. A phase‐1‐2 study.
1983 • 60 citations
GABA Receptors and Phospholipids
1978 • 59 citations
Sex differences in the response of rats to drugs affecting GABAergic transmission
1985 • 59 citations
Kinetics of open channel block by penicillin of single GABAA receptor channels from mouse spinal cord neurones in culture.
1992 • 58 citations
Glycine and spinal inhibition
1967 • 58 citations
Antibodies Specific for α‐Subunit Subtypes of GABAA Receptors Reveal Brain Regional Heterogeneity
1993 • 58 citations
Enhancement by anesthetic and convulsant barbiturates of GABA binding to rat brain synaptosomal membranes
1981 • 58 citations
Avermectin Bla Modulation of γ‐Aminobutyric Acid/Benzodiazepine Receptor Binding in Mammalian Brain
1985 • 58 citations
Activation of Calcium‐Phospholipid‐Dependent Protein Kinase Enhances Benzodiazepine and Barbiturate Potentiation of the GABAA Receptor
1993 • 57 citations
Adrenalectomy Selectively Regulates GABAA Receptor Subunit Expression in the Hippocampus
1994 • 56 citations
Sex difference in response to alphaxalone anaesthesia may be oestrogen dependent
1982 • 56 citations
Effects of fenamates and other nonsteroidal anti-inflammatory drugs on rat brain GABAA receptors expressed in Xenopus oocytes.
1994 • 55 citations
GABA triggers a Cl− efflux from cultured mouse oligodendrocytes
1989 • 55 citations
Ethanol inhibits a neuronal ATP-gated ion channel.
1993 • 54 citations
[Effect of diazepam on presynaptic inhibition and other spinal reflexes].
1967 • 54 citations
Synthesis and Photochemistry of Photolabile Derivatives of .gamma.-Aminobutyric Acid for Chemical Kinetic Investigations of the .gamma.-Aminobutyric Acid Receptor in the Millisecond Time Region
1994 • 54 citations
Transamination of analogues of γ-aminobutyric acid by extracts of rat brain mitochondria
1973 • 54 citations
Actions of avermectin B1a on the γ‐aminobutyric AcidA receptor and chloride channels in rat brain
1986 • 53 citations
Benzodiazepine Suppression of Cortisol Secretion: A Measure of Anxiolytic Activity?
1986 • 53 citations
Ammonia potentiates GABAA response in dissociated rat cortical neurons
1993 • 52 citations
4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogs of THIP. Synthesis and biological activity
1983 • 52 citations
GABA?The quintessential neurotransmitter: Electroneutrality, fidelity, specificity, and a model for the ligand binding site of GABAA receptors
1993 • 51 citations
Etomidate potentiation of GABAA receptor gated current depends on the subunit composition
1995 • 51 citations
Thermodynamics of gamma-aminobutyric acid type A receptor binding differentiate agonists from antagonists.
1994 • 51 citations
THE PHYSIOLOGICAL ACTION OF CHOLESTEROL
1927 • 51 citations
Antagonism by penicillin of γ-aminobutyric acid depolarizations at presynaptic sites in rat olfactory cortex and cuneate nucleus in vitro
1980 • 51 citations
Sex and strain differences in GABA receptor binding after chronic ethanol drinking in mice
1980 • 50 citations
Muscimol and the uptake of ?-aminobutyric acid by rat brain slices
1971 • 50 citations
Neurochemical Studies on Quinolone Antibiotics: Effects on Glutamate, GABA and Adenosine Systems in Mammalian CNS
1989 • 49 citations
Pregnenolone—from selye to Alzheimer and a model of the pregnenolone sulfate binding site on the GABAA receptor
1995 • 48 citations
New developments on the search for the endogenous ligand(s) of central benzodiazepine receptors
1988 • 48 citations
GABA agonists. Resolution, absolute stereochemistry and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol
1985 • 47 citations
Bidirectional effects of benzodiazepine receptor ligands against picrotoxin- and pentylenetetrazol-induced seizures
1983 • 47 citations
Molecular Determinants of General Anesthetic Action: Role of GABAA Receptor Structure
1993 • 46 citations
Currents Activated by GABA and their Modulation by Zn2+ in Cerebellar Granule Cells in Culture
1993 • 46 citations
Antagonism of inhibitory amino acids by the steroid derivative RU5135
1985 • 45 citations
Testosterone Enhances GABA and Taurine but not N‐Methyl‐D,L‐Aspartate Stimulation of Gonadotropin Secretion in the Goldfish: Possible Sex Steroid Feedback Mechanisms
1993 • 45 citations
Flavonoids from Leptospermum scoparium with affinity to the benzodiazepine receptor characterized by structure activity relationships and in vivo studies of a plant extract.
1994 • 45 citations
Steroids and neuronal activity
1991 • 44 citations
Effects of 5-HT3 receptor antagonists on binding and function of mouse and human GABAA receptors
1994 • 44 citations
Functional Heterogeneity of Hippocampal GABAA Receptors
1993 • 44 citations
Phospholipid Methylation Increases [3H]Diazepam and [3H]GABA Binding in Membrane Preparations of Rat Cerebellum
1983 • 43 citations
Effects of Antiepileptic Drugs on GABA Responses and on Reduction of GABA Responses by PTZ and DMCM on Mouse Neurons in Cell Culture
1989 • 43 citations
Sex Differences in the Effects of Acute Swim Stress on Binding to GABAA Receptors in Mouse Brain
1993 • 43 citations
Electrophysiological studies of the GABAA receptor ligand, 4‐PIOL, on cultured hippocampal neurones
1991 • 42 citations
Neurosteroid analogs: structure-activity studies of benz[e]indene modulators of GABAA receptor function. 1. The effect of 6-methyl substitution on the electrophysiological activity of 7-substituted benz[e]indene-3-carbonitriles
1993 • 42 citations
Gamma-aminobutyric acidA receptor function is inhibited by microtubule depolymerization.
1994 • 40 citations
Interactions between three pyridazinyl-GABA derivatives and central GABA and glycine receptors in the rat, an in vivo microiontophoretic study
1986 • 39 citations
Phospholipids and benzodiazepine recognition sites of brain synaptic membranes
1981 • 38 citations
Bidirectional Modulation of GABA‐Gated Chloride Channels by Divalent Cations: Inhibition by Ca2+ and Enhancement by Mg2+
1994 • 38 citations
Convulsant doses of penicillin shorten the lifetime of GABA‐induced channels in cultured central neurones
1986 • 38 citations
Purines interact with ‘central’ but not ‘peripheral’ benzodiazepine binding sites
1982 • 37 citations
Cortisol: A potent biphasic modulator at GABAA-receptor complexes in the guinea pig isolated ileum
1987 • 37 citations
.alpha.-Spirocyclopentyl- and .alpha.-spirocyclopropyl-.gamma.-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant .alpha.,.alpha.-disubstituted .gamma.-butyrolactones
1994 • 36 citations
Selective effects of dieldrin on the GABAA receptor-channel subunits expressed in human embryonic kidney cells
1994 • 36 citations
Ovarian steroid modulation of [3H]muscimol binding in the spinal cord of the rat
1991 • 35 citations
Pharmacology of Neurosteroid Biosynthesis. Role of the Mitochondrial DBI Receptor (MDR) Complex
1994 • 35 citations
Time course of GABA and glycine actions on cat spinal neurones: Effect of pentobarbitone
1978 • 35 citations
Selective potentiation of GABA-mediated Cl− current by lanthanum ion in subtypes of cloned GABAA receptors
1992 • 34 citations
Stress — the neglected variable in experimental pharmacology and toxicology
1987 • 34 citations
Characterization of GAVAA receptor-mediated 36chloride uptake in rat brain synaptoneurosomes
1987 • 34 citations
DL-Tetrazol-5-ylglycine, a highly potent NMDA agonist: its synthesis and NMDA receptor efficacy
1992 • 34 citations
(+)‐Hydrastine, a potent competitive antagonist at mammalian GABAA receptors
1990 • 33 citations
Evidence for association of a high affinity avermectin binding site with the benzodiazepine receptor
1984 • 33 citations
CoMFA validation of the superposition of six classes of compounds which block GABA receptors non-competitively
1993 • 33 citations
GABA‐Mimetic Activity and Effects on Diazepam Binding of Aminosulphonic Acids Structurally Related to Piperidine‐4‐Sulphonic Acid
1985 • 33 citations
Effects of diuretics on GABA‐gated chloride current in frog isolated sensory neurones
1988 • 32 citations
Effects of pentylenetetrazol on GABA-A/benzodiazepine/picrotoxinin receptor complexes in rat brain regions
1986 • 31 citations
Isothiouronium compounds as γ‐aminobutyric acid agonists
1986 • 31 citations
The GABA agonist THIP, attenuates antinociception in the mouse by modifying central cholinergic transmission
1987 • 31 citations
Functional changes in GABAA receptor stimulation during the oestrous cycle of the rat
1991 • 30 citations
Differences in the interactions between GABA and benzodiazepine binding sites
1982 • 30 citations
Liposome‐entrapped GABA modifies behavioral and electrographic changes of penicillin‐induced epileptic activity
1982 • 30 citations
Purine inhibition of [3H]-γ-aminobutyric acid receptor binding to rat brain membranes
1980 • 30 citations
Regulation of gaba receptor binding to synaptic plasma membrane of rat cerebral cortex: The role of endogenous phospholipids
1981 • 29 citations
Comparison of the analgesic actions of THIP and morphine
1983 • 29 citations
A comparison of the actions of pentobarbitone and etomidate on [3H]GABA binding to crude synaptosomal rat brain membranes
1981 • 29 citations
Bicuculline blocks nicotinic acetylcholine response in isolated intermediate lobe cells of the pig
1991 • 29 citations
GABA‐A agonists and GABA uptake inhibitors: Structure‐activity relationships
1990 • 29 citations
The GABAA receptor channel mediated chloride ion translocation through the plasma membrane: New insights from 36Cl− ion flux measurements
1993 • 29 citations
Pyridazinyl-GABA derivatives as GABA and glycine antagonists in the spinal cord of the cat
1986 • 29 citations
Bromide, in the therapeutic concentration, enhances GABA-activated currents in cultured neurons of rat cerebral cortex
1994 • 28 citations
The effects of anaesthetic and convulsant barbiturates on the efflux of [3H]d-aspartate from brain minislices
1980 • 28 citations
Inhibition of Glutamate Release by Arachidonic Acid in Rat Cerebrocortical Synaptosomes
1991 • 28 citations
Inhibition of acetylcholinesterase by bicuculline and related alkaloids
1975 • 28 citations
Binding interactions of convulsant and anticonvulsant gamma-butyrolactones and gamma-thiobutyrolactones with the picrotoxin receptor.
1990 • 28 citations
Neonatal stress and long-term modulation of GABA receptors in rat brain
1990 • 27 citations
γ-Aminobutyric acid receptor binding antagonism by the amidine steroid RU5135
1984 • 27 citations
Taurine allosterically modulates flunitrazepam binding to synaptic membranes
1992 • 27 citations
Sex differences in GABAA receptor binding in rat brain measured by an improved in vitro binding assay
1990 • 27 citations
Voltage-dependent modulation of GABAA receptor channel desensitization in rat hippocampal neurons
1994 • 27 citations
Glycine antagonism by RU 5135
1985 • 26 citations
Comparative Photoaffinity Labeling Study between Azidophenyl, Difluoroazidophenyl, and Tetrafluoroazidophenyl Derivatives for the GABA-Gated Chloride Channels
1995 • 26 citations
Activation of Cl? channels by avermectin in rat cultured hippocampal neurons
1993 • 26 citations
Diazotization and Thiocyanate Differentiate Agonists from Antagonists for the High‐ and Low‐Affinity Receptors of γ‐Aminobutyric Acid
1984 • 26 citations
Pentobarbitone slows the dissociation of GABA from rat brain synaptosomal binding sites
1981 • 25 citations
Contrasting regulation by GABA of the displacement of benzodiazepine antagonist binding by benzodiazepine agonists and purines
1982 • 25 citations
Mono N-Aryl ethylenediamine and piperazine derivatives are GABAA receptor blockers: Implications for psychiatry
1993 • 25 citations
Inhibition of [methyl-3H]diazepam binding to rat brain membranes in vitro by dinatin and skrofulein.
1994 • 24 citations
On the GABAA receptor: A molecular modeling approach
1989 • 24 citations
Influence of membrane potential on conductance sublevels of chloride channels activated by GABA
1994 • 24 citations
Effects of Amitriptyline on GABA-stimulated 36Cl− uptake in relation to a behavioral model of depression
1995 • 24 citations
GABA RECEPTORS: AS COMPLEX AS ABC?
1994 • 24 citations
Synthesis of Analogues of GABA. III. All Four Stereoisomers of 3-Aminocyclopentanecarboxylic Acid and a Stereochemical Correlation with Amidinomycin
1979 • 24 citations
δ-Guanidinovaleric acid as an endogenous and specific GABA-receptor antagonist: electroencephalographic study
1987 • 23 citations
Effects of taurine on cell morphology and expression of low-affinity GABA receptors in cultured cerebellar granule cells
1989 • 23 citations
Effects of 5-hydroxytryptamine on central neurones antagonized by bicuculline and picrotoxin
1981 • 23 citations
Diazepam stimulates the binding of GABA and muscimol but not thip to rat brain membranes
1983 • 23 citations
Modulatory action of arachidonic acid on GABAA/chloride channel receptor function in adult and aged brain cortex membranes
1993 • 23 citations
Gamma-butyrolactone antagonism of the picrotoxin receptor: comparison of a pure antagonist and a mixed antagonist/inverse agonist.
1991 • 23 citations
Endogenous inhibitors of picrotoxinin-convulsant binding sites in rat brain
1980 • 22 citations
Modification of responses to sensory and hippocampal stimuli in neurons of the rat mediobasal hypothalamus in the presence of iontophoretically applied cortisol
1981 • 22 citations
Alkyl-substituted γ-butyrolactones act at a distinct site allosterically linked to the TBPS/picrotoxinin site on the GABAA receptor complex
1993 • 21 citations
Water-soluble steroidal anaesthetics
1979 • 21 citations
γ‐Aminobutyric Acid Receptor Ionophore Complexes: Differential Effects of Deltamethrin, Dichlorodiphenyltrichloroethane, and Some Novel Insecticides in a Rat Brain Membrane Preparation
1987 • 20 citations
Activation of γ‐aminobutyric acid insensitive chloride channels in mouse brain synaptic vesicles by avermectin B1a
1991 • 20 citations
Corticosteroid receptors and the central nervous system
1994 • 20 citations
Benzodiazepines and barbiturate potentiate the pre- and postsynaptic gamma-aminobutyric acid (GABA)A receptor-mediated response in the enteric nervous system of guinea pig small intestine.
1988 • 19 citations
Brain Region-Specific Effects of Neuroactive Steroids on the Affinity and Density of the GABA-Binding Site
1993 • 19 citations
Interaction of pitrazepin with the GABA/benzodiazepine receptor complex and with glycine receptors
1985 • 19 citations
Reductions in blood pressure, heart rate and renal sympathetic nervous discharge after imidazole-4-acetic acid: mediation through central gamma-aminobutyric acid (GABA) receptor stimulation.
1981 • 18 citations
Indomethacin/ibuprofen-like anti-inflammatory agents selectively potentiate the gamma-aminobutyric acid-antagonistic effects of several norfloxacin-like quinolone antibacterial agents on [35S]t-butylbicyclophosphorothionate binding.
1993 • 18 citations
Synthesis and pharmacological characterization of l-trans-4-tetrazolylproline (ly300020): A novel systemically-active ampa receptor agonist
1993 • 18 citations
Cortisone: a potent GABAA antagonist in the guinea-pig isolated ileum
1990 • 18 citations
Beware the builders: Construction noise changes [14C]GABA release and uptake from amygdaloid and hippocampal slices in the rat
1993 • 18 citations
Modulation of [3H]flunitrazepam binding to rat cerebellar benzodiazepine receptors by phosphatidylserine
1987 • 17 citations
Pregnenolone and its sulphate modulate GABAA-receptor-mediated contractile responses in the guinea-pig isolated ileum
1987 • 17 citations
Increased γ‐Aminobutyric Acid Receptor Function in the Cerebral Cortex of Myoclonic Calves with an Hereditary Deficit in Glycine/Strychnine Receptors
1990 • 17 citations
Direct excitant action of convulsant barbiturates
1981 • 17 citations
Actions of pentobarbitone and derivatives with modified 5-butyl substituents on GABA and diazepam binding to rat brain synaptosomal membranes
1983 • 16 citations
GABA activated chloride currents in cultured rat hippocampal and septal region neurons can be inhibited by curare and atropine
1988 • 16 citations
Radioautographic Evidence that the GABAA Receptor Antagonist SR 95531 is a Substrate Inhibitor of MAO‐A in the Rat and Human Locus Coeruleus
1994 • 16 citations
Novel arylaminopyridazine-GABA receptor antagonists examined electrophysiologically in Ascaris suum
1995 • 16 citations
Effects of cortisol on GABAA receptor-mediated responses compared in guinea-pig ileum and rat cuneate nucleus
1989 • 16 citations
Benzodiazepines and steroidogenesis
1992 • 16 citations
Picrodendrins, a New Group of Picrotoxane Terpenoids: Structure-Activity Profile of Action at the GABAAReceptor-coupled Picrotoxinin Binding Site in Rat Brain
1994 • 15 citations
Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum
1991 • 15 citations
GABA<scp>a</scp> AGONISTS AS TARGETS FOR DRUG DEVELOPMENT
1992 • 14 citations
ZAPA, (Z)‐3‐[(aminoiminomethyl)thio]‐2‐propenoic acid hydrochloride, a potent agonist at GABA‐receptors on the Ascaris muscle cell
1988 • 14 citations
The bicuculline - like properties of dopamine sulfate in rat brain
1984 • 13 citations
Interaction of La3+ with GABAA receptors in rat cerebrocortical membranes as detected with [35S]t-butylbicyclophosphorothionate binding
1993 • 13 citations
Thiomuscimol, a new photoaffinity label for the GABAA receptor
1995 • 13 citations
Diazepam enhances the action but not the binding of the GABA analog, THIP
1984 • 13 citations
Cyclic GABA-GABOB analogues. IV. Activity on learning and memory.
1984 • 13 citations
Penicillin‐induced potentiation of glycine receptor‐operated choride current in rat ventro‐medial hypothalamic neurones
1992 • 12 citations
Modulation of the GABAA-like autoreceptor by barbiturates but not by steroids
1993 • 11 citations
Zur Physiologie und Pharmakologie der Sterine
1936 • 11 citations
Amino acid antagonists and the depression of cuneate neurones by -aminobutyric acid (GABA) and glycine.
1973 • 11 citations
Astroglia‐released factor shows similar effects as benzodiazepine inverse agonists
1994 • 11 citations
Methods for removing endogenous factors from CNS membrane preparations: Differences in [3H]GABA binding parameters and developmental-related effects
1993 • 10 citations
Barbiturates and calcium-activated adenosine triphosphatase
1979 • 10 citations
m‐Sulfonate Benzene Diazonium Chloride: A Powerful Affinity Label for the γ‐Aminobutyric Acid Binding Site from Rat Brain
1992 • 10 citations
U-93631 causes rapid decay of gamma-aminobutyric acid-induced chloride currents in recombinant rat gamma-aminobutyric acid type A receptors.
1993 • 10 citations
ZAPA, a substrate for the neuronal high affinity GABA uptake system in rat brain slices
1991 • 10 citations
Strychnine-insensitive glycine binding to cerebral cortical membranes in developing and ageing mice
1993 • 10 citations
Inhibition of GABAA receptor-mediated current responses by enoxacin (new quinolone) and felbinac (non-steroidal anti-inflammatory drug) in Xenopus oocytes injected with mouse-brain messenger RNA.
1993 • 9 citations
Selective blockade of benzodiazepine receptors by Ro 15-1788 prevents foot shock-induced decrease of low affinity γ-aminobutyric acid receptors
1985 • 9 citations
2-Imino-1,3,4-thiadiazole Derivatives of GABA as GABAA Antagonists
1990 • 9 citations
Pitrazepin: a central glycine and GABA antagonist
1986 • 9 citations
Synergistic effect of phosphatidylserine with ?-aminobutyric acid in antagonizing the isoniazid-induced convulsions in mice
1984 • 9 citations
Electrophysiological and metabolic effects of a convulsant barbiturate on dissociated mouse primary sensory neurons.
1995 • 8 citations
Benzodiazepine Receptor Ligands with Positive and Negative Efficacy
1984 • 8 citations
Convulsant effects of cunaniol, a polyacetylenic alcohol isolated from the plant Clibadium sylvestre, on frogs and mice
1969 • 8 citations
An antinociceptive profile of kojic amine: An analogue of γ-aminobutyric acid (GABA)
1987 • 8 citations
Gamma-aminobutyric acidA receptor function is modulated by cyclic GMP
1995 • 8 citations
Isolation of endogenous modulators for the GABAA and taurine receptors
1993 • 7 citations
Does bicuculline antagonize NMDA receptors? Further evidence in the rat striatum
1994 • 7 citations
Effects of gamma-aminobutyric acid on the compound action potential of the rat superior cervical ganglion.
1993 • 7 citations
Sodium-Independent, High-Affinity Binding of [3H]γ-Aminobutyric Acid in Human Neurological Disorders
1979 • 7 citations
In Vivo Formation of Benzodiazepine-like Molecules in Mammalian Brain
1993 • 6 citations
Bis(2-chloroalkyl)amides of Acylated Amino Acids. Modified Nitrogen Mustards1
1965 • 5 citations
Cannabinoid metabolite interacts with benzodiazepine receptor
1992 • 5 citations
Structural factors governing agonist and antagonist activity in the GABAA system
1988 • 5 citations
Penicilin-induced triphasic modulation of GABAA receptor-operated chloride current in frog sensory neuron
1992 • 5 citations
Caprolactam-barbiturate interaction at the GABAA receptor complex in the guinea-pig intestine
1986 • 5 citations
Differential modulation of γ-aminobutyric acid receptors by caprolactam derivatives with central nervous system depressant on convulsant activity
1985 • 5 citations
Synthesis of Substituted (+)-Bicuculline Derivatives Through Chloromethylation
1990 • 5 citations
m-Sulphonate benzene diazonium chloride: A novel GABAA receptor antagonist
1994 • 4 citations
Effects of a depressant/convulsant pair of glutarimides on neuronal activity in the isolated spinal cord of the immature rat
1985 • 3 citations
The synthesis of 1,8-disubstituted 10,11-dihydrodibenz[b,f]oxepin-10-ones. analogues of anaesthetic steroids
1991 • 3 citations
Formation of γ‐Amino‐β‐Hydroxybutyric Acid from 2‐Hydroxyputrescine in Rat Brain
1988 • 3 citations
Effect of phosphatidylserine on the basal and GABA-activated Cl? permeation across single nerve membranes from rabbit Deiters' neurons
1990 • 2 citations
Esters of 6‐(4′‐fluorobenzylamino)‐β‐ carboline‐3‐carboxylic acid as potential benzodiazepine imaging agents for P.E.T.
1995 • 1 citations