Page last updated: 2024-08-24

tiagabine and nipecotic acid

tiagabine has been researched along with nipecotic acid in 23 studies

Research

Studies (23)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's6 (26.09)18.2507
2000's7 (30.43)29.6817
2010's9 (39.13)24.3611
2020's1 (4.35)2.80

Authors

AuthorsStudies
Borden, LA; Branchek, TA; Dhar, TG; Gluchowski, C; Smith, KE; Tyagarajan, S; Weinshank, RL1
Bruno-Blanch, L; Gálvez, J; García-Domenech, R1
Höfner, G; Kragler, A; Wanner, KT1
Faust, MR; Höfner, G; Pabel, J; Wanner, KT1
Lutz, TA; Petrera, M; Sindelar, M; Wanner, KT1
Höfner, G; Quandt, G; Wanner, KT1
Hellenbrand, T; Höfner, G; Wanner, KT; Wein, T1
Kern, F; Wanner, KT1
Lambert, JD; Roepstorff, A1
Chapman, AG; Meldrum, BS; Parvez, NS; Smith, SE1
Andersen, KE; Braestrup, C; Grønwald, FC; Jørgensen, AS; Knutsen, LJ; Nielsen, EB; Sonnewald, U; Suzdak, PD; Sørensen, PO1
Draguhn, A; Heinemann, U; Meierkord, H; Pfeiffer, M1
Egebjerg, J; Sørensen, PO; Thomsen, C1
Scholze, P; Singer, EA; Sitte, HH1
Kreil, A; Richter, A1
Fang, K; Lin, G; Liu, X; Zhang, J; Zhang, P1
Bräuner-Osborne, H; Jørgensen, FS; Skovstrup, S; Taboureau, O1
David, L; Jørgensen, FS; Skovstrup, S; Taboureau, O1
Akhtar, MJ; Bhatia, R; Kumar, B; Kumar, P; Mehta, V; Singh, K1
Dörnyei, G; Gács-Baitz, E; Héja, L; Incze, M; Kardos, J; Kovács, I; Peredy-Kajtár, M; Szántay, C; Szárics, E; Temesváriné-Major, E1
Guo, L; Jiang, H; Lin, G; Luo, X; Wen, R; Xu, L; Zhang, J; Zheng, J1
Borkar, N; Clausen, RP; Jørgensen, L; Krogsgaard-Larsen, P; Madsen, KK; Schousboe, A; Skovgaard-Petersen, J; Vogensen, SB; Wellendorph, P; White, HS1
Dine, J; Eder, M; Höfner, G; Lutz, T; Pabel, J; Wanner, KT; Wein, T1

Reviews

1 review(s) available for tiagabine and nipecotic acid

ArticleYear
Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies.
    European journal of medicinal chemistry, 2022, Apr-15, Volume: 234

    Topics: Anticonvulsants; GABA Uptake Inhibitors; gamma-Aminobutyric Acid; Humans; Nipecotic Acids; Tiagabine

2022

Other Studies

22 other study(ies) available for tiagabine and nipecotic acid

ArticleYear
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.
    Journal of medicinal chemistry, 1994, Jul-22, Volume: 37, Issue:15

    Topics: Animals; Binding Sites; Biological Transport; Blood-Brain Barrier; Carrier Proteins; Cell Line; Cloning, Molecular; Drug Design; GABA Antagonists; GABA Plasma Membrane Transport Proteins; gamma-Aminobutyric Acid; Humans; Ligands; Membrane Proteins; Membrane Transport Proteins; Nipecotic Acids; Organic Anion Transporters; Proline; Rats

1994
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
    Bioorganic & medicinal chemistry letters, 2003, Aug-18, Volume: 13, Issue:16

    Topics: Anticonvulsants; Computer Simulation; Databases, Factual; Discriminant Analysis; Drug Design; Molecular Structure; Quantitative Structure-Activity Relationship

2003
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.
    European journal of medicinal chemistry, 2008, Volume: 43, Issue:11

    Topics: Animals; Benzylamines; Cell Line; GABA Plasma Membrane Transport Proteins; GABA Uptake Inhibitors; gamma-Aminobutyric Acid; Humans; Methylation; Mice; Molecular Structure; Structure-Activity Relationship

2008
Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.
    European journal of medicinal chemistry, 2010, Volume: 45, Issue:6

    Topics: Animals; Azetidines; Biological Transport; Cattle; GABA Plasma Membrane Transport Proteins; GABA Uptake Inhibitors; gamma-Aminobutyric Acid; Inhibitory Concentration 50; Structure-Activity Relationship

2010
Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.
    Journal of medicinal chemistry, 2013, Feb-14, Volume: 56, Issue:3

    Topics: GABA Plasma Membrane Transport Proteins; Hydrazones; Mass Spectrometry

2013
Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.
    Bioorganic & medicinal chemistry, 2013, Jun-01, Volume: 21, Issue:11

    Topics: Animals; Anticonvulsants; Biological Transport; Cell Membrane; GABA Plasma Membrane Transport Proteins; GABA Uptake Inhibitors; gamma-Aminobutyric Acid; HEK293 Cells; Humans; Mice; Neuroprotective Agents; Nipecotic Acids; Structure-Activity Relationship; Vinyl Compounds

2013
Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors.
    Bioorganic & medicinal chemistry, 2016, May-01, Volume: 24, Issue:9

    Topics: Drug Evaluation, Preclinical; GABA Uptake Inhibitors; Nipecotic Acids

2016
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.
    Bioorganic & medicinal chemistry, 2019, 04-01, Volume: 27, Issue:7

    Topics: Binding Sites; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Enzyme Inhibitors; HEK293 Cells; Humans; Mass Spectrometry; Molecular Structure; N-Acetylglucosaminyltransferases; Oximes; Small Molecule Libraries; Structure-Activity Relationship

2019
Comparison of the effect of the GABA uptake blockers, tiagabine and nipecotic acid, on inhibitory synaptic efficacy in hippocampal CA1 neurones.
    Neuroscience letters, 1992, Nov-09, Volume: 146, Issue:2

    Topics: Animals; GABA Antagonists; gamma-Aminobutyric Acid; Hippocampus; In Vitro Techniques; Kinetics; Male; Neurons; Nipecotic Acids; Proline; Rats; Rats, Wistar; Synapses; Synaptic Transmission; Tiagabine

1992
The gamma-aminobutyric acid uptake inhibitor, tiagabine, is anticonvulsant in two animal models of reflex epilepsy.
    European journal of pharmacology, 1995, Feb-06, Volume: 273, Issue:3

    Topics: Acoustic Stimulation; Animals; Anticonvulsants; Behavior, Animal; Carbamazepine; Epilepsy; Female; GABA Agents; Male; Motor Activity; Myoclonus; Neurotransmitter Uptake Inhibitors; Nicotinic Acids; Nipecotic Acids; Oximes; Papio; Photic Stimulation; Proline; Rats; Rats, Inbred Strains; Tiagabine

1995
The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate.
    Journal of medicinal chemistry, 1993, Jun-11, Volume: 36, Issue:12

    Topics: Animals; Anticonvulsants; GABA Antagonists; gamma-Aminobutyric Acid; Molecular Structure; Nicotinic Acids; Nipecotic Acids; Proline; Prosencephalon; Rats; Stereoisomerism; Structure-Activity Relationship; Synaptosomes; Tiagabine

1993
Effects of gamma-aminobutyric acid (GABA) agonists and GABA uptake inhibitors on pharmacosensitive and pharmacoresistant epileptiform activity in vitro.
    British journal of pharmacology, 1996, Volume: 119, Issue:3

    Topics: Animals; Baclofen; Dose-Response Relationship, Drug; Entorhinal Cortex; Epilepsy; Female; GABA Agonists; gamma-Aminobutyric Acid; Hippocampus; In Vitro Techniques; Magnesium; Male; Membrane Potentials; Muscimol; Neurons; Neurotransmitter Uptake Inhibitors; Nipecotic Acids; Proline; Rats; Rats, Wistar; Tiagabine

1996
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.
    British journal of pharmacology, 1997, Volume: 120, Issue:6

    Topics: Animals; Carrier Proteins; Cell Line; Cricetinae; GABA Plasma Membrane Transport Proteins; gamma-Aminobutyric Acid; Membrane Proteins; Membrane Transport Proteins; Mice; Neurotransmitter Uptake Inhibitors; Nipecotic Acids; Organic Anion Transporters; Piperidines; Proline; Tiagabine

1997
Bi-directional transport of GABA in human embryonic kidney (HEK-293) cells stably expressing the rat GABA transporter GAT-1.
    British journal of pharmacology, 2002, Volume: 135, Issue:1

    Topics: Aminobutyrates; Animals; Biological Transport, Active; Carrier Proteins; Cell Line; Cells, Cultured; Dose-Response Relationship, Drug; Drug Interactions; GABA Antagonists; GABA Plasma Membrane Transport Proteins; gamma-Aminobutyric Acid; Gene Expression; Humans; Kidney; Membrane Proteins; Membrane Transport Proteins; Nerve Tissue Proteins; Neurotransmitter Uptake Inhibitors; Nipecotic Acids; Organic Anion Transporters; Ouabain; Rats; Receptors, GABA; Tiagabine; Tritium

2002
Antidystonic efficacy of gamma-aminobutyric acid uptake inhibitors in the dtsz mutant.
    European journal of pharmacology, 2005, Oct-03, Volume: 521, Issue:1-3

    Topics: Animals; Cricetinae; Disease Progression; Dose-Response Relationship, Drug; Dystonia; Female; GABA Antagonists; Injections, Intraperitoneal; Male; Mutation; Nipecotic Acids; Oximes; Random Allocation; Severity of Illness Index; Tiagabine; Time Factors; Treatment Outcome

2005
Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors.
    Bioorganic & medicinal chemistry letters, 2007, Jul-01, Volume: 17, Issue:13

    Topics: Animals; Anticonvulsants; Carboxylic Acids; Chemistry, Pharmaceutical; Drug Design; GABA Antagonists; GABA Plasma Membrane Transport Proteins; gamma-Aminobutyric Acid; Imidazoles; Inhibitory Concentration 50; Mice; Models, Chemical; Nipecotic Acids; Piperidines; Structure-Activity Relationship; Temperature; Tiagabine

2007
Homology modelling of the GABA transporter and analysis of tiagabine binding.
    ChemMedChem, 2010, Jul-05, Volume: 5, Issue:7

    Topics: Amino Acid Sequence; Anticonvulsants; Binding Sites; Drug Design; GABA Plasma Membrane Transport Proteins; Humans; Molecular Dynamics Simulation; Molecular Sequence Data; Nipecotic Acids; Sequence Alignment; Structural Homology, Protein; Tiagabine

2010
A steered molecular dynamics study of binding and translocation processes in the GABA transporter.
    PloS one, 2012, Volume: 7, Issue:6

    Topics: Anticonvulsants; Binding Sites; Cytoplasm; GABA Plasma Membrane Transport Proteins; gamma-Aminobutyric Acid; Humans; Kinetics; Ligands; Models, Molecular; Molecular Conformation; Molecular Dynamics Simulation; Nipecotic Acids; Protein Binding; Protein Conformation; Tiagabine

2012
Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
    Journal of medicinal chemistry, 2004, Nov-04, Volume: 47, Issue:23

    Topics: Amino Acids; Animals; Biological Transport; Brain; Ergolines; Excitatory Amino Acid Antagonists; GABA Antagonists; gamma-Aminobutyric Acid; Glutamic Acid; In Vitro Techniques; Male; Models, Molecular; Radioligand Assay; Rats; Rats, Wistar; Stereoisomerism; Structure-Activity Relationship

2004
Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).
    Bioorganic & medicinal chemistry letters, 2006, Jan-01, Volume: 16, Issue:1

    Topics: Animals; Biological Transport; Carboxylic Acids; Chemistry, Pharmaceutical; Drug Design; Drug Evaluation, Preclinical; GABA Agonists; gamma-Aminobutyric Acid; Humans; Inhibitory Concentration 50; Models, Chemical; Neurons; Nipecotic Acids; Pipecolic Acids; Structure-Activity Relationship; Tiagabine

2006
Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization.
    Journal of medicinal chemistry, 2013, Mar-14, Volume: 56, Issue:5

    Topics: Animals; Cells, Cultured; GABA Plasma Membrane Transport Proteins; GABA Uptake Inhibitors; Inhibitory Concentration 50; Isoxazoles; Mice; Neurons

2013
Development of New Photoswitchable Azobenzene Based γ-Aminobutyric Acid (GABA) Uptake Inhibitors with Distinctly Enhanced Potency upon Photoactivation.
    Journal of medicinal chemistry, 2018, 07-26, Volume: 61, Issue:14

    Topics: Azo Compounds; Biological Transport; gamma-Aminobutyric Acid; HEK293 Cells; Humans; Molecular Docking Simulation; N-Acetylglucosaminyltransferases; Nipecotic Acids; Photochemical Processes; Protein Conformation; Structure-Activity Relationship

2018