Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile.

[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 .