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64603-91-4,MFCD00242754
Catalog No.:AA006T12

64603-91-4 | Gaboxadol hydrochloride

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250mg
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1g
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA006T12
Chemical Name:
Gaboxadol hydrochloride
CAS Number:
64603-91-4
Molecular Formula:
C6H9ClN2O2
Molecular Weight:
176.6009
MDL Number:
MFCD00242754
SMILES:
O=c1[nH]oc2c1CCNC2.Cl
Properties
Properties
 
Storage:
2-8℃;Light sensitive;  

Computed Properties
 
Complexity:
210  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
10  
Hydrogen Bond Acceptor Count:
3  
Hydrogen Bond Donor Count:
2  
XLogP3:
-0.9  

Literature

Title: Synergistic antidepressant-like action of gaboxadol and escitalopram.

Journal: European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology 20121001

Title: Function and expression of the proton-coupled amino acid transporter PAT1 along the rat gastrointestinal tract: implications for intestinal absorption of gaboxadol.

Journal: British journal of pharmacology 20121001

Title: Intestinal drug transport via the proton-coupled amino acid transporter PAT1 (SLC36A1) is inhibited by Gly-X(aa) dipeptides.

Journal: Molecular pharmaceutics 20120904

Title: Positive modulation of δ-subunit containing GABA(A) receptors in mouse neurons.

Journal: Neuropharmacology 20120901

Title: Effect of ganaxolone and THIP on operant and limited-access ethanol self-administration.

Journal: Neuropharmacology 20120901

Title: Tonic inhibition enhances fidelity of sensory information transmission in the cerebellar cortex.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20120808

Title: Enhanced slow wave sleep and improved sleep maintenance after gaboxadol administration during seven nights of exposure to a traffic noise model of transient insomnia.

Journal: Journal of psychopharmacology (Oxford, England) 20120801

Title: EEG spectral power density profiles during NREM sleep for gaboxadol and zolpidem in patients with primary insomnia.

Journal: Journal of psychopharmacology (Oxford, England) 20120801

Title: Combining escitalopram with gaboxadol provides no additional benefit in the treatment of patients with severe major depressive disorder.

Journal: The international journal of neuropsychopharmacology 20120701

Title: The role of GABAergic system on the inhibitory effect of ghrelin on food intake in neonatal chicks.

Journal: Neuroscience letters 20120627

Title: Carrier-mediated γ-aminobutyric acid transport across the basolateral membrane of human intestinal Caco-2 cell monolayers.

Journal: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V 20120601

Title: Modulation of spinal GABAergic analgesia by inhibition of chloride extrusion capacity in mice.

Journal: The journal of pain : official journal of the American Pain Society 20120601

Title: Benzodiazepines modulate GABAA receptors by regulating the preactivation step after GABA binding.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20120425

Title: Knockout of the γ-aminobutyric acid receptor subunit α4 reduces functional δ-containing extrasynaptic receptors in hippocampal pyramidal cells at the onset of puberty.

Journal: Brain research 20120423

Title: Upregulation of high-affinity GABA(A) receptors in cultured rat dorsal root ganglion neurons.

Journal: Neuroscience 20120419

Title: GABA site agonist gaboxadol induces addiction-predicting persistent changes in ventral tegmental area dopamine neurons but is not rewarding in mice or baboons.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20120411

Title: Effect of Mimosa pudica (Linn.) extract on anxiety behaviour and GABAergic regulation of 5-HT neuronal activity in the mouse.

Journal: Journal of psychopharmacology (Oxford, England) 20120401

Title: Intracellular chloride concentration influences the GABAA receptor subunit composition.

Journal: Nature communications 20120313

Title: Effects of general anaesthetics on 5-HT neuronal activity in the dorsal raphe nucleus.

Journal: Neuropharmacology 20120301

Title: GABAA-positive modulator selective discriminative stimulus effects of 1,1,1-trichloroethane vapor.

Journal: Drug and alcohol dependence 20120201

Title: Tonic GABAA receptor conductance in medial subnucleus of the tractus solitarius neurons is inhibited by activation of μ-opioid receptors.

Journal: Journal of neurophysiology 20120201

Title: Targeting the restricted α-subunit repertoire of airway smooth muscle GABAA receptors augments airway smooth muscle relaxation.

Journal: American journal of physiology. Lung cellular and molecular physiology 20120115

Title: Prion protein is a key determinant of alcohol sensitivity through the modulation of N-methyl-D-aspartate receptor (NMDAR) activity.

Journal: PloS one 20120101

Title: Neurosteroid influences on sensitivity to ethanol.

Journal: Frontiers in endocrinology 20120101

Title: [Post partum depression: future perspectives].

Journal: Rivista di psichiatria 20120101

Title: Effects of GABAB ligands alone and in combination with paroxetine on hippocampal BDNF gene expression.

Journal: European journal of pharmacology 20111205

Title: The SLC36 family of proton-coupled amino acid transporters and their potential role in drug transport.

Journal: British journal of pharmacology 20111201

Title: Gi-coupled γ-aminobutyric acid-B receptors cross-regulate phospholipase C and calcium in airway smooth muscle.

Journal: American journal of respiratory cell and molecular biology 20111201

Title: Alteration of ethanol drinking in mice via modulation of the GABA(A) receptor with ganaxolone, finasteride, and gaboxadol.

Journal: Alcoholism, clinical and experimental research 20111101

Title: EEG power spectra response to a 4-h phase advance and gaboxadol treatment in 822 men and women.

Journal: Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine 20111015

Title: Molecular basis for the high THIP/gaboxadol sensitivity of extrasynaptic GABA(A) receptors.

Journal: Journal of neurophysiology 20111001

Title: Reduced postsynaptic GABAA receptor number and enhanced gaboxadol induced change in holding currents in Purkinje cells of the dystrophin-deficient mdx mouse.

Journal: Neurobiology of disease 20110901

Title: Differential modulatory actions of GABAA agonists on susceptibility to GABAA antagonists-induced seizures in morphine dependent rats: possible mechanisms in seizure propensity.

Journal: Pharmacology, biochemistry, and behavior 20110701

Title: Selective GABA transporter inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABA(A) receptor agonist gaboxadol.

Journal: The Journal of pharmacology and experimental therapeutics 20110701

Title: The 4-aminopyridine in vitro epilepsy model analyzed with a perforated multi-electrode array.

Journal: Neuropharmacology 20110601

Title: Sex-specificity of associative learning-induced changes in GABAergic tonic inhibition in layer 4 neurons of mouse barrel cortex.

Journal: Behavioural brain research 20110601

Title: Pharmacological enhancement of δ-subunit-containing GABA(A) receptors that generate a tonic inhibitory conductance in spinal neurons attenuates acute nociception in mice.

Journal: Pain 20110601

Title: Neurosteroid modulation of benzodiazepine-sensitive GABAA tonic inhibition in supraoptic magnocellular neurons.

Journal: American journal of physiology. Regulatory, integrative and comparative physiology 20110601

Title: Residual effects of esmirtazapine on actual driving performance: overall findings and an exploratory analysis into the role of CYP2D6 phenotype.

Journal: Psychopharmacology 20110501

Title: Hippocampal GABAergic dysfunction in a rat chronic mild stress model of depression.

Journal: Hippocampus 20110401

Title: Tonic extrasynaptic GABA(A) receptor currents control gonadotropin-releasing hormone neuron excitability in the mouse.

Journal: Endocrinology 20110401

Title: Non-neuronal, slow GABA signalling in the ventrobasal thalamus targets δ-subunit-containing GABA(A) receptors.

Journal: The European journal of neuroscience 20110401

Title: Extrasynaptic GABAA receptor activation reverses recognition memory deficits in an animal model of schizophrenia.

Journal: Psychopharmacology 20110301

Title: Pharmacologic Treatment with GABA(B) Receptor Agonist of Methamphetamine-Induced Cognitive Impairment in Mice.

Journal: Current neuropharmacology 20110301

Title: Gaboxadol has affinity for the proton-coupled amino acid transporter 1, SLC36A1 (hPAT1)--A modelling approach to determine IC(50) values of the three ionic species of gaboxadol.

Journal: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20110214

Title: Pharmacology of structural changes at the GABA(A) receptor transmitter binding site.

Journal: British journal of pharmacology 20110201

Title: Differential effects of two major neurosteroids on cerebellar and cortical GABA(A) receptor binding and function.

Journal: European journal of pharmacology 20110110

Title: Amino acid derivatives are substrates or non-transported inhibitors of the amino acid transporter PAT2 (slc36a2).

Journal: Biochimica et biophysica acta 20110101

Title: Extrasynaptic GABA(A) receptors and tonic inhibition in rat auditory thalamus.

Journal: PloS one 20110101

Title: Standard operation procedures for conducting the on-the-road driving test, and measurement of the standard deviation of lateral position (SDLP).

Journal: International journal of general medicine 20110101

Title: Augmentation of Tonic GABA(A) Inhibition in Absence Epilepsy: Therapeutic Value of Inverse Agonists at Extrasynaptic GABA(A) Receptors.

Journal: Advances in pharmacological sciences 20110101

Title: Removal of GABA(A) receptor γ2 subunits from parvalbumin neurons causes wide-ranging behavioral alterations.

Journal: PloS one 20110101

Title: A Comparison of the α2/3/5 Selective Positive Allosteric Modulators L-838,417 and TPA023 in Preclinical Models of Inflammatory and Neuropathic Pain.

Journal: Advances in pharmacological sciences 20110101

Title: Role of anticonvulsant and antiepileptogenic neurosteroids in the pathophysiology and treatment of epilepsy.

Journal: Frontiers in endocrinology 20110101

Title: Sex differences and the effect of gaboxadol and zolpidem on EEG power spectra in NREM and REM sleep.

Journal: Journal of psychopharmacology (Oxford, England) 20101101

Title: The neurosteroid dehydroepiandrosterone (DHEA) and its metabolites alter 5-HT neuronal activity via modulation of GABAA receptors.

Journal: Journal of psychopharmacology (Oxford, England) 20101101

Title: Alterations in cyclic alternating pattern associated with phase advanced sleep are differentially modulated by gaboxadol and zolpidem.

Journal: Sleep 20101101

Title: The proton-coupled amino acid transporter, SLC36A1 (hPAT1), transports Gly-Gly, Gly-Sar and other Gly-Gly mimetics.

Journal: British journal of pharmacology 20101001

Title: Defective GABAergic neurotransmission and pharmacological rescue of neuronal hyperexcitability in the amygdala in a mouse model of fragile X syndrome.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20100721

Title: Pulvinar inactivation disrupts selection of movement plans.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20100623

Title: Diversity of structure and function of alpha1alpha6beta3delta GABAA receptors: comparison with alpha1beta3delta and alpha6beta3delta receptors.

Journal: The Journal of biological chemistry 20100604

Title: Increase of GABAA receptor-mediated tonic inhibition in dentate granule cells after traumatic brain injury.

Journal: Neurobiology of disease 20100601

Title: Distinct activities of GABA agonists at synaptic- and extrasynaptic-type GABAA receptors.

Journal: The Journal of physiology 20100415

Title: Prototypic GABA(A) receptor agonist muscimol acts preferentially through forebrain high-affinity binding sites.

Journal: Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20100301

Title: Effect of gaboxadol on patient-reported measures of sleep and waking function in patients with Primary Insomnia: results from two randomized, controlled, 3-month studies.

Journal: Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine 20100215

Title: 5-Hydroxy-L-tryptophan alters gaboxadol pharmacokinetics in rats: involvement of PAT1 and rOat1 in gaboxadol absorption and elimination.

Journal: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20100131

Title: Mice lacking Gad2 show altered behavioral effects of ethanol, flurazepam and gabaxadol.

Journal: Addiction biology 20100101

Title: Pharmacological characterization of a novel positive modulator at alpha 4 beta 3 delta-containing extrasynaptic GABA(A) receptors.

Journal: Neuropharmacology 20100101

Title: A graphical vector autoregressive modelling approach to the analysis of electronic diary data.

Journal: BMC medical research methodology 20100101

Title: Sleep and recovery in physicians on night call: a longitudinal field study.

Journal: BMC health services research 20100101

Title: Distinct α subunit variations of the hypothalamic GABAA receptor triplets (αβγ) are linked to hibernating state in hamsters.

Journal: BMC neuroscience 20100101

Title: Highway driving performance and cognitive functioning the morning after bedtime and middle-of-the-night use of gaboxadol, zopiclone and zolpidem.

Journal: Journal of sleep research 20091201

Title: Structure of alpha6 beta3 delta GABA(A) receptors and their lack of ethanol sensitivity.

Journal: Journal of neurochemistry 20091201

Title: Progesterone and allopregnanolone enhance the miniature synaptic release of glycine in the rat hypoglossal nucleus.

Journal: The European journal of neuroscience 20091201

Title: Brain regional distribution of GABA(A) receptors exhibiting atypical GABA agonism: roles of receptor subunits.

Journal: Neurochemistry international 20091101

Title: Neonatal allopregnanolone increases novelty-directed locomotion and disrupts behavioural responses to GABA(A) receptor modulators in adulthood.

Journal: International journal of developmental neuroscience : the official journal of the International Society for Developmental Neuroscience 20091001

Title: A 2-week efficacy and safety study of gaboxadol and zolpidem using electronic diaries in primary insomnia outpatients.

Journal: Sleep medicine 20090801

Title: Intestinal gaboxadol absorption via PAT1 (SLC36A1): modified absorption in vivo following co-administration of L-tryptophan.

Journal: British journal of pharmacology 20090801

Title: Tolerance to sedative/hypnotic actions of GABAergic drugs correlates with tolerance to potentiation of extrasynaptic tonic currents of alcohol-dependent rats.

Journal: Journal of neurophysiology 20090701

Title: Dissociating anxiolytic and sedative effects of GABAAergic drugs using temperature and locomotor responses to acute stress.

Journal: Psychopharmacology 20090601

Title: Regulation of light's action in the mammalian circadian clock: role of the extrasynaptic GABAA receptor.

Journal: American journal of physiology. Regulatory, integrative and comparative physiology 20090501

Title: The effects of agonists of ionotropic GABA(A) and metabotropic GABA(B) receptors on learning.

Journal: The Spanish journal of psychology 20090501

Title: Quantitative microdialysis using modified ultraslow microdialysis: direct rapid and reliable determination of free brain concentrations with the MetaQuant technique.

Journal: Journal of neuroscience methods 20090415

Title: Inhibition of thalamic excitability by 4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridine-3-ol: a selective role for delta-GABA(A) receptors.

Journal: The European journal of neuroscience 20090301

Title: Metabolism and renal elimination of gaboxadol in humans: role of UDP-glucuronosyltransferases and transporters.

Journal: Pharmaceutical research 20090201

Title: Tolerability, pharmacokinetics and night-time effects on postural sway and critical flicker fusion of gaboxadol and zolpidem in elderly subjects.

Journal: British journal of clinical pharmacology 20090201

Title: GABAB receptor agonist baclofen improves methamphetamine-induced cognitive deficit in mice.

Journal: European journal of pharmacology 20090105

Title: Next-day residual effects of gaboxadol and flurazepam administered at bedtime: a randomized double-blind study in healthy elderly subjects.

Journal: Human psychopharmacology 20090101

Title: Understanding your inhibitions: effects of GABA and GABAA receptor modulation on brain cortical metabolism.

Journal: Journal of neurochemistry 20090101

Title: The influence of agonists of GABA(A) and GABA(B) receptors on the formation of the defensive and inhibitory conditioned reflexes.

Journal: Doklady biological sciences : proceedings of the Academy of Sciences of the USSR, Biological sciences sections 20090101

Title: Comparison of the novel subtype-selective GABAA receptor-positive allosteric modulator NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem, bretazenil, and gaboxadol in rat models of inflammatory and neuropathic pain.

Journal: The Journal of pharmacology and experimental therapeutics 20081201

Title: K+ channel TASK-1 knockout mice show enhanced sensitivities to ataxic and hypnotic effects of GABA(A) receptor ligands.

Journal: The Journal of pharmacology and experimental therapeutics 20081001

Title: Effect of gaboxadol on sleep in adult and elderly patients with primary insomnia: results from two randomized, placebo-controlled, 30-night polysomnography studies.

Journal: Sleep 20081001

Title: Neuropharmacology.

Journal: Indian journal of pharmacology 20081001

Title: Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.

Journal: Journal of medicinal chemistry 20080814

Title: Tonically active inhibition selectively controls feedforward circuits in mouse barrel cortex.

Journal: Journal of neurophysiology 20080801

Title: GABAA receptor modulation in dorsal root ganglia in vivo affects chronic pain after nerve injury.

Journal: Neuroscience 20080717

Title: Perinatal alcohol exposure leads to prolonged upregulation of hypothalamic GABA A receptors and increases behavioral sensitivity to gaboxadol.

Journal: Neuroscience letters 20080711

Title: Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.

Journal: Journal of medicinal chemistry 20080710

Title: Gaboxadol -- a different hypnotic profile with no tolerance to sleep EEG and sedative effects after repeated daily dosing.

Journal: Pharmacology, biochemistry, and behavior 20080701

Title: Cell type-specific GABA A receptor-mediated tonic inhibition in mouse neocortex.

Journal: Journal of neurophysiology 20080701

Title: Impaired GABAergic transmission disrupts normal homeostatic plasticity in rat cortical networks.

Journal: The European journal of neuroscience 20080601

Title: Effect of microdialysis perfusion of 4,5,6,7-tetrahydroisoxazolo-[5,4-c]pyridine-3-ol in the perifornical hypothalamus on sleep-wakefulness: role of delta-subunit containing extrasynaptic GABAA receptors.

Journal: Neuroscience 20080515

Title: Efficacy of the selective extrasynaptic GABA A agonist, gaboxadol, in a model of transient insomnia: a randomized, controlled clinical trial.

Journal: Sleep medicine 20080501

Title: Discriminative stimulus effects of tiagabine and related GABAergic drugs in rats.

Journal: Psychopharmacology 20080501

Title: Slow wave sleep enhancement with gaboxadol reduces daytime sleepiness during sleep restriction.

Journal: Sleep 20080501

Title: Enhanced behavioral sensitivity to the competitive GABA agonist, gaboxadol, in transgenic mice over-expressing hippocampal extrasynaptic alpha6beta GABA(A) receptors.

Journal: Journal of neurochemistry 20080401

Title: The role of GABA(A) receptors in the control of transient lower oesophageal sphincter relaxations in the dog.

Journal: British journal of pharmacology 20080301

Title: GABA(A) receptors in normal development and seizures: friends or foes?

Journal: Current neuropharmacology 20080301

Title: The expression of GABAA beta subunit isoforms in synaptic and extrasynaptic receptor populations of mouse dentate gyrus granule cells.

Journal: The Journal of physiology 20080215

Title: Sleep-stabilizing effects of E-6199, compared to zopiclone, zolpidem and THIP in mice.

Journal: Sleep 20080201

Title: Functional consequences of GABAA receptor alpha 4 subunit deletion on synaptic and extrasynaptic currents in mouse dentate granule cells.

Journal: Alcoholism, clinical and experimental research 20080101

Title: Epilepsy, E/I Balance and GABA(A) Receptor Plasticity.

Journal: Frontiers in molecular neuroscience 20080101

Title: GABA(A) Receptor Dynamics and Constructing GABAergic Synapses.

Journal: Frontiers in molecular neuroscience 20080101

Title: Short-term treatment with gaboxadol improves sleep maintenance and enhances slow wave sleep in adult patients with primary insomnia.

Journal: Psychopharmacology 20071101

Title: GABAergic modulation of binge-like ethanol intake in C57BL/6J mice.

Journal: Pharmacology, biochemistry, and behavior 20071101

Title: Identification of a domain in the delta subunit (S238-V264) of the alpha4beta3delta GABAA receptor that confers high agonist sensitivity.

Journal: Journal of neurochemistry 20071101

Title: Development and validation of a selective and sensitive bioanalytical procedure for the quantitative determination of gaboxadol in human plasma employing mixed mode solid phase extraction and hydrophilic interaction liquid chromatography with tandem mass spectroscopic detection.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20071015

Title: Neurochemical regulation of sleep.

Journal: Journal of psychiatric research 20071001

Title: Postnatal development and kinetics of [3H]gaboxadol binding in rat brain: in vitro homogenate binding and quantitative autoradiography.

Journal: Brain research 20070919

Title: 5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.

Journal: Journal of medicinal chemistry 20070823

Title: Flumazenil selectively prevents the increase in alpha(4)-subunit gene expression and an associated change in GABA(A) receptor function induced by ethanol withdrawal.

Journal: Journal of neurochemistry 20070801

Title: Dual GABAA receptor-mediated inhibition in rat presympathetic paraventricular nucleus neurons.

Journal: The Journal of physiology 20070715

Title: Lack of generalisation between the GABAA receptor agonist, gaboxadol, and allosteric modulators of the benzodiazepine binding site in the rat drug discrimination procedure.

Journal: Psychopharmacology 20070701

Title: New perspectives for the treatment of disorders of sleep and arousal.

Journal: Annales pharmaceutiques francaises 20070701

Title: The importance of genetic background on pain behaviours and pharmacological sensitivity in the rat spared serve injury model of peripheral neuropathic pain.

Journal: European journal of pharmacology 20070614

Title: Plasma and CNS concentrations of Gaboxadol in rats following subcutaneous administration.

Journal: European journal of pharmacology 20070507

Title: GABAA receptors in the thalamus: alpha4 subunit expression and alcohol sensitivity.

Journal: Alcohol (Fayetteville, N.Y.) 20070501

Title: The selective extrasynaptic GABAA agonist, gaboxadol, improves traditional hypnotic efficacy measures and enhances slow wave activity in a model of transient insomnia.

Journal: Sleep 20070501

Title: KCC2-deficient mice show reduced sensitivity to diazepam, but normal alcohol-induced motor impairment, gaboxadol-induced sedation, and neurosteroid-induced hypnosis.

Journal: Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20070401

Title: Gaboxadol, a selective extrasynaptic GABA(A) agonist, does not generalise to other sleep-enhancing drugs: a rat drug discrimination study.

Journal: Neuropharmacology 20070301

Title: Modulation of extrasynaptic THIP conductances by GABAA-receptor modulators in mouse neocortex.

Journal: Journal of neurophysiology 20070301

Title: The EEG effects of THIP (Gaboxadol) on sleep and waking are mediated by the GABA(A)delta-subunit-containing receptors.

Journal: The European journal of neuroscience 20070301

Title: Effect of short-term treatment with gaboxadol on sleep maintenance and initiation in patients with primary insomnia.

Journal: Sleep 20070301

Title: A single point mutation of the GABA(A) receptor alpha5-subunit confers fluoxetine sensitivity.

Journal: Neuropharmacology 20070201

Title: Auto-modulation of neuroactive steroids on GABA A receptors: a novel pharmacological effect.

Journal: Neuropharmacology 20070201

Title: The progesterone metabolite allopregnanolone potentiates GABA(A) receptor-mediated inhibition of 5-HT neuronal activity.

Journal: European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology 20070115

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20070101

Title: Mechanisms of sleep induction by GABA(A) receptor agonists.

Journal: The Journal of clinical psychiatry 20070101

Title: [New hypnotics: perspectives from sleep physiology].

Journal: Vertex (Buenos Aires, Argentina) 20070101

Title: Treating insomnia: Current and investigational pharmacological approaches.

Journal: Pharmacology & therapeutics 20061201

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20061001

Title: Deletion of the GABA(A) receptor alpha1 subunit increases tonic GABA(A) receptor current: a role for GABA uptake transporters.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20060906

Title: THIP, a hypnotic and antinociceptive drug, enhances an extrasynaptic GABAA receptor-mediated conductance in mouse neocortex.

Journal: Cerebral cortex (New York, N.Y. : 1991) 20060801

Title: delta-Subunit containing GABAA receptor knockout mice are less sensitive to the actions of 4,5,6,7-tetrahydroisoxazolo-[5,4-c]pyridin-3-ol.

Journal: European journal of pharmacology 20060717

Title: Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds.

Journal: Journal of medicinal chemistry 20060713

Title: Steroid withdrawal in the mouse results in anxiogenic effects of 3alpha,5beta-THP: a possible model of premenstrual dysphoric disorder.

Journal: Psychopharmacology 20060601

Title: Discriminative stimulus effects of flumazenil: perceptual masking by baclofen, and lack of substitution with gamma-hydroxybutyrate and its precursors 1,4-butanediol and gamma-butyrolactone.

Journal: Behavioural pharmacology 20060501

Title: Extrasynaptic GABAA receptors are critical targets for sedative-hypnotic drugs.

Journal: Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine 20060415

Title: Sleep circuitry and the hypnotic mechanism of GABAA drugs.

Journal: Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine 20060415

Title: Pharmacological characterisation of place escape/avoidance behaviour in the rat chronic constriction injury model of neuropathic pain.

Journal: Psychopharmacology 20060401

Title: Pharmacological characterization of agonists at delta-containing GABAA receptors: Functional selectivity for extrasynaptic receptors is dependent on the absence of gamma2.

Journal: The Journal of pharmacology and experimental therapeutics 20060301

Title: Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.

Journal: Journal of medicinal chemistry 20060223

Title: Involvement of GABAergic modulation of antinociception induced by morphine microinjected into the ventrolateral orbital cortex.

Journal: Brain research 20060216

Title: Chronic intermittent ethanol-induced switch of ethanol actions from extrasynaptic to synaptic hippocampal GABAA receptors.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20060208

Title: Gaboxadol--a new awakening in sleep.

Journal: Current opinion in pharmacology 20060201

Title: Impact of epsilon and theta subunits on pharmacological properties of alpha3beta1 GABAA receptors expressed in Xenopus oocytes.

Journal: BMC pharmacology 20060101

Title: GABAA receptor-mediated tonic inhibition in thalamic neurons.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20051214

Title: An extrasynaptic GABAA receptor mediates tonic inhibition in thalamic VB neurons.

Journal: Journal of neurophysiology 20051201

Title: Sleep disturbances, psychiatric disorders, and psychotropic drugs.

Journal: Dialogues in clinical neuroscience 20051201

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20051101

Title: Short-term steroid treatment increases delta GABAA receptor subunit expression in rat CA1 hippocampus: pharmacological and behavioral effects.

Journal: Neuropharmacology 20051001

Title: Ischemic tolerance induction in organotypic hippocampal slices: role for the GABA(A) receptor?

Journal: Neuroscience letters 20050801

Title: Distinct patterns of expression and regulation of GABA receptors containing the delta subunit in cerebellar granule and hippocampal neurons.

Journal: Journal of neurochemistry 20050801

Title: Centrally-mediated antinociceptive actions of GABA(A) receptor agonists in the rat spared nerve injury model of neuropathic pain.

Journal: European journal of pharmacology 20050601

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20050601

Title: Effects of gabaergic drugs on reserpine-induced oral dyskinesia.

Journal: Behavioural brain research 20050507

Title: Calcium-stimulated adenylyl cyclases are critical modulators of neuronal ethanol sensitivity.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20050420

Title: Effect of repeated gaboxadol administration on night sleep and next-day performance in healthy elderly subjects.

Journal: Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20050401

Title: Combined discriminative stimulus effects of midazolam with other positive GABAA modulators and GABAA receptor agonists in rhesus monkeys.

Journal: Psychopharmacology 20050401

Title: Internalized GABA-receptor subunits are transferred to an intracellular pool associated with the postsynaptic density.

Journal: The European journal of neuroscience 20050101

Title: Charged residues at the 2' position of human GABAC rho 1 receptors invert ion selectivity and influence open state probability.

Journal: The Journal of biological chemistry 20041224

Title: GABA receptor modulation of 5-HT neuronal firing: characterization and effect of moderate in vivo variations in glucocorticoid levels.

Journal: Neurochemistry international 20041201

Title: Over-expression of the fyn-kinase gene reduces hypnotic sensitivity to ethanol in mice.

Journal: Neuroscience letters 20041130

Title: Compounds exhibiting selective efficacy for different beta subunits of human recombinant gamma-aminobutyric acid A receptors.

Journal: The Journal of pharmacology and experimental therapeutics 20041101

Title: GABA pharmacology--what prospects for the future?

Journal: Biochemical pharmacology 20041015

Title: GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.

Journal: Biochemical pharmacology 20041015

Title: Altered pharmacology of synaptic and extrasynaptic GABAA receptors on CA1 hippocampal neurons is consistent with subunit changes in a model of alcohol withdrawal and dependence.

Journal: The Journal of pharmacology and experimental therapeutics 20040901

Title: Antagonism by NOS inhibition of the behavioral effects of benzodiazepine and GABAA receptor agonists in the mouse elevated plus-maze.

Journal: Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20040801

Title: Gaboxadol. Lundbeck/Merck.

Journal: Current opinion in investigational drugs (London, England : 2000) 20040701

Title: Deletion of the fyn-kinase gene alters sensitivity to GABAergic drugs: dependence on beta2/beta3 GABAA receptor subunits.

Journal: The Journal of pharmacology and experimental therapeutics 20040601

Title: Activation of single heteromeric GABA(A) receptor ion channels by full and partial agonists.

Journal: The Journal of physiology 20040601

Title: Effects of a low dose of ethanol in an animal model of premenstrual anxiety.

Journal: Alcohol (Fayetteville, N.Y.) 20040501

Title: Estradiol and testosterone modulate the anesthetic action of the GABA-A agonist THIP, but not of the neurosteroid 3alpha,5beta-pregnanolone in the rat.

Journal: Psychopharmacology 20040301

Title: Changes in rectal temperature and ECoG spectral power of sensorimotor cortex elicited in conscious rabbits by i.c.v. injection of GABA, GABA(A) and GABA(B) agonists and antagonists.

Journal: British journal of pharmacology 20040101

Title: Anticonvulsant and antiepileptogenic effects of GABAA receptor ligands in pentylenetetrazole-kindled mice.

Journal: Progress in neuro-psychopharmacology & biological psychiatry 20040101

Title: Rotarod studies in the rat of the GABAA receptor agonist gaboxadol: lack of ethanol potentiation and benzodiazepine cross-tolerance.

Journal: European journal of pharmacology 20031215

Title: Aza-THIP and related analogues of THIP as GABA C antagonists.

Journal: Bioorganic & medicinal chemistry 20031117

Title: Evidence for inhibitory effect of the agonist gaboxadol at human alpha 1 beta 2 gamma 2S GABAA receptors.

Journal: European journal of pharmacology 20030930

Title: Extrasynaptic GABA(A) channels activated by THIP are modulated by diazepam in CA1 pyramidal neurons in the rat brain hippocampal slice.

Journal: Molecular and cellular neurosciences 20030901

Title: Pharmacology of GABA(A) receptors exhibiting different levels of spontaneous activity.

Journal: European journal of pharmacology 20030822

Title: The GABAA receptor agonist THIP is neuroprotective in organotypic hippocampal slice cultures.

Journal: Brain research 20030530

Title: Gaboxadol: in vitro interaction studies with benzodiazepines and ethanol suggest functional selectivity.

Journal: European journal of pharmacology 20030425

Title: Progesterone withdrawal increases the anxiolytic actions of gaboxadol: role of alpha4betadelta GABA(A) receptors.

Journal: Neuroreport 20030120

Title: Deletion of the alpha1 or beta2 subunit of GABAA receptors reduces actions of alcohol and other drugs.

Journal: The Journal of pharmacology and experimental therapeutics 20030101

Title: Gamma-aminobutyric acid-induced calcium signalling in rat superior collicular neurones.

Journal: Neuroscience letters 20021213

Title: Prenatal protein malnutrition enhances stimulus control by CDP, but not a CDP/THIP combination in rats.

Journal: Pharmacology, biochemistry, and behavior 20021101

Title: Characterization of GABA(A) receptor ligands in the rat cortical wedge preparation: evidence for action at extrasynaptic receptors?

Journal: British journal of pharmacology 20020901

Title: Discovery of non-zwitterionic GABA(A) receptor full agonists and a superagonist.

Journal: Bioorganic & medicinal chemistry letters 20020805

Title: GABA(A) receptor ligands and their therapeutic potentials.

Journal: Current topics in medicinal chemistry 20020801

Title: Medicinal chemistry and molecular pharmacology of GABA(C) receptors.

Journal: Current topics in medicinal chemistry 20020801

Title: Discriminative stimulus effects of ethanol in C57BL/6J and DBA/2J inbred mice.

Journal: Alcoholism, clinical and experimental research 20020601

Title: Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.

Journal: The Journal of biological chemistry 20020419

Title: Inhibition of THIP on morphine-induced hyperactivity, reverse tolerance and postsynaptic dopamine receptor supersensitivity.

Journal: Archives of pharmacal research 20020401

Title: trans-4-Amino-2-methylbut-2-enoic acid (2-MeTACA) and (+/-)-trans-2-aminomethylcyclopropanecarboxylic acid ((+/-)-TAMP) can differentiate rat rho3 from human rho1 and rho2 recombinant GABA(C) receptors.

Journal: British journal of pharmacology 20020201

Title: Opposite roles of GABA and excitatory amino acids on the control of GAD expression in cultured retina cells.

Journal: Brain research 20020118

Title: Characterisation of rat superficial superior colliculus neurones: firing properties and sensitivity to GABA.

Journal: Neuroscience 20020101

Title: Early compensation of vestibulo-oculomotor symptoms after unilateral vestibular loss in rats is related to GABA(B) receptor function.

Journal: Neuroscience 20020101

Title: GABAergic and glutamatergic terminals differentially influence the organization of GABAergic synapses in rat cerebellar granule cells in vitro.

Journal: Neuroscience 20020101

Title: Specific GABA(A) agonists and partial agonists.

Journal: Chemical record (New York, N.Y.) 20020101

Title: Microscopic kinetics and energetics distinguish GABA(A) receptor agonists from antagonists.

Journal: Biophysical journal 20011101

Title: The GABA(A) agonist gaboxadol improves the quality of post-nap sleep.

Journal: Psychopharmacology 20010901

Title: Effect of the GABAA agonist gaboxadol on nocturnal sleep and hormone secretion in healthy elderly subjects.

Journal: American journal of physiology. Endocrinology and metabolism 20010701

Title: Effects of GABA(A) receptor partial agonists in primary cultures of cerebellar granule neurons and cerebral cortical neurons reflect different receptor subunit compositions.

Journal: British journal of pharmacology 20010601

Title: Entropy as the predominant driving force of binding to human recombinant alpha(x)beta(3)gamma(2) GABA(A) receptors.

Journal: European journal of pharmacology 20010105

Title: The GABA uptake inhibitor tiagabine promotes slow wave sleep in normal elderly subjects.

Journal: Neurobiology of aging 20010101

Title: Involvement of GABAergic neurotransmission in the neurobiology of the apomorphine-induced aggressive behavior paradigm, a model of psychotic behavior in rats.

Journal: Methods and findings in experimental and clinical pharmacology 20001001

Title: Hyperalgesic effect induced by barbiturates, midazolam and ethanol: pharmacological evidence for GABA-A receptor involvement.

Journal: Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas 19970201

Title: Effect of manipulation of the GABA system on dopamine-related behaviors.

Journal: Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas 19950101

Title: Pharmacology of GABA rho 1 and GABA alpha/beta receptors expressed in Xenopus oocytes and COS cells.

Journal: British journal of pharmacology 19930501

Title: Relative anticonvulsant effects of GABAmimetic and GABA modulatory agents.

Journal: Epilepsia 19920101

Title: [Antiabstinent action of fenibut and baclofen on a model of abstinence induced by the benzodiazepine receptor antagonist CGS 8216 in rats receiving diazepam].

Journal: Biulleten' eksperimental'noi biologii i meditsiny 19870601

Title: Hoestgaard-Jensen K, et al. Probing α4βδ GABAA receptor heterogeneity: differential regional effects of a functionally selective α4β1δ/α4β3δ receptor agonist on tonic and phasic inhibition in rat brain. J Neurosci. 2014 Dec 3;34(49):16256-72.

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