Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile.
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A. Schousboe | R. Clausen | H. Bräuner‐Osborne | T. Kvist | S. B. Vogensen | K. Madsen | A. Jensen | Lars Jørgensen | Bolette Kragholm | Karsten K. Madsen
[1] Arne Schousboe,et al. Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization. , 2013, Journal of medicinal chemistry.
[2] K. Harpsøe,et al. Discovery of a Novel Allosteric Modulator of 5-HT3 Receptors , 2012, The Journal of Biological Chemistry.
[3] U. Gether,et al. SLC6 Neurotransmitter Transporters: Structure, Function, and Regulation , 2011, Pharmacological Reviews.
[4] A. Schousboe,et al. Selective GABA Transporter Inhibitors Tiagabine and EF1502 Exhibit Mechanistic Differences in Their Ability to Modulate the Ataxia and Anticonvulsant Action of the Extrasynaptic GABAA Receptor Agonist Gaboxadol , 2011, Journal of Pharmacology and Experimental Therapeutics.
[5] T. Liljefors,et al. GABA and Glutamate Receptor Ligands and their Therapeutic Potential in CNS Disorders , 2010 .
[6] A. Schousboe,et al. Synaptic and extrasynaptic GABA transporters as targets for anti‐epileptic drugs , 2009, Journal of neurochemistry.
[7] H. Bräuner‐Osborne,et al. The four human gamma-aminobutyric acid (GABA) transporters: pharmacological characterization and validation of a highly efficient screening assay. , 2009, Combinatorial chemistry & high throughput screening.
[8] J. Kehler,et al. Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. , 2009, Journal of medicinal chemistry.
[9] J. Bauer,et al. Tiagabine: efficacy and safety in partial seizures – current status , 2008, Neuropsychiatric disease and treatment.
[10] A. Schousboe,et al. Inhibition of the betaine-GABA transporter (mGAT2/BGT-1) modulates spontaneous electrographic bursting in the medial entorhinal cortex (mEC) , 2008, Epilepsy Research.
[11] A. Meinild,et al. Cloning and Characterization of a Functional Human γ-Aminobutyric Acid (GABA) Transporter, Human GAT-2* , 2007, Journal of Biological Chemistry.
[12] Harel Weinstein,et al. A Comprehensive Structure-Based Alignment of Prokaryotic and Eukaryotic Neurotransmitter/Na+ Symporters (NSS) Aids in the Use of the LeuT Structure to Probe NSS Structure and Function , 2006, Molecular Pharmacology.
[13] Arne Schousboe,et al. Structure-activity relationships of selective GABA uptake inhibitors. , 2006, Current topics in medicinal chemistry.
[14] Arne Schousboe,et al. A novel selective γ-aminobutyric acid transport inhibitor demonstrates a functional role for GABA transporter subtype GAT2/BGT-1 in the CNS , 2006, Neurochemistry International.
[15] P. Zwanzger,et al. Selective GABAergic treatment for panic? Investigations in experimental panic induction and panic disorder. , 2005, Journal of psychiatry & neuroscience : JPN.
[16] Arne Schousboe,et al. Selective inhibitors of GABA uptake: synthesis and molecular pharmacology of 4-N-methylamino-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol analogues. , 2005, Bioorganic & medicinal chemistry.
[17] Scott Slough,et al. First Demonstration of a Functional Role for Central Nervous System Betaine/γ-Aminobutyric Acid Transporter (mGAT2) Based on Synergistic Anticonvulsant Action among Inhibitors of mGAT1 and mGAT2 , 2005, Journal of Pharmacology and Experimental Therapeutics.
[18] L. Jasmin,et al. GABA puts a stop to pain. , 2004, Current drug targets. CNS and neurological disorders.
[19] J. Coyle. The GABA-glutamate connection in schizophrenia: which is the proximate cause? , 2004, Biochemical pharmacology.
[20] F. Conti,et al. GABA transporters in the mammalian cerebral cortex: localization, development and pathological implications , 2004, Brain Research Reviews.
[21] A. A. Jensen,et al. Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay. , 2004, Biochemical pharmacology.
[22] M. Reith,et al. Synaptic uptake and beyond: the sodium- and chloride-dependent neurotransmitter transporter family SLC6 , 2004, Pflügers Archiv.
[23] P. Brambilla,et al. GABAergic dysfunction in mood disorders , 2003, Molecular Psychiatry.
[24] H. Lester,et al. GABA transporter-1 (GAT1)-deficient mice: differential tonic activation of GABAA versus GABAB receptors in the hippocampus. , 2003, Journal of neurophysiology.
[25] Arne Schousboe,et al. Correlation between Anticonvulsant Activity and Inhibitory Action on Glial γ-Aminobutyric Acid Uptake of the Highly Selective Mouse γ-Aminobutyric Acid Transporter 1 Inhibitor 3-Hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and ItsN-Alkylated Analogs , 2002, Journal of Pharmacology and Experimental Therapeutics.
[26] D. Treiman. GABAergic Mechanisms in Epilepsy , 2001, Epilepsia.
[27] P. Genton,et al. Tiagabine in Clinical Practice , 2001, Epilepsia.
[28] Thomas D. Y. Chung,et al. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays , 1999, Journal of biomolecular screening.
[29] C. Thomsen,et al. 1‐(3‐(9H‐Carbazol‐9‐yl)‐1‐propyl)‐4‐(2‐methoxyphenyl)‐4‐piperidinol, a novel subtype selective inhibitor of the mouse type II GABA‐transporter , 1997, British journal of pharmacology.
[30] F. Lombardo,et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings , 1997 .
[31] P. Suzdak,et al. A Review of the Preclinical Pharmacology of Tiagabine: A Potent and Selective Anticonvulsant GABA Uptake Inhibitor , 1995, Epilepsia.
[32] T. Branchek,et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. , 1994, European journal of pharmacology.
[33] P. Suzdak,et al. (R)‐N‐[4,4‐Bis(3‐Methyl‐2‐Thienyl)but‐3‐en‐1‐yl]Nipecotic Acid Binds with High Affinity to the Brain γ‐Aminobutyric Acid Uptake Carrier , 1990, Journal of neurochemistry.
[34] A. Schousboe,et al. GABA uptake inhibitors: relevance to antiepileptic drug research , 1987, Epilepsy Research.
[35] A. Schousboe,et al. Effect of Homo‐β‐Proline and Other Heterocyclic GAB A Analogues on GABA Uptake in Neurons and Astroglial Cells and on GABA Receptor Binding , 1981, Journal of neurochemistry.
[36] O. Snead,et al. GABA, γ‐hydroxybutyric acid, and neurological disease , 2003 .