Bente Frølund
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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3-hydroxyisoxazole bioiosteres of gaba - synthesis of a series of 4-substituted muscimol analogs and identification of a bicyclic 2-isoxazoline rearrangement product
Hjeds, H., Christensen, I. T., Cornett, Claus, Frølund, Bente, Falch, E., Pedersen, J. B. & Krogsgaardlarsen, P., 1992, In: Acta Chemica Scandinavica. Supplementum. 46, 8, p. 772-777 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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4-Hydroxy-1,2,3-triazole moiety as bioisostere of the carboxylic acid function: a novel scaffold to probe the orthosteric gamma-aminobutyric acid receptor binding site
Alessandro, G., Krall, J., Nielsen, Birgitte, Sørensen, T. E., Kongstad, Kenneth Thermann, Barbara, R., Donatella, B., Frølund, Bente & Lolli, M. L., 5 Oct 2018, In: European Journal of Medicinal Chemistry. 158, p. 311-321 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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4-PIOL, a low-efficacy partial GABA-A agonist
Frølund, Bente, Kristiansen, Uffe, Nathan, T., Falch, E., Lambert, J. D. C. & Krogsgaard-Larsen, Povl, 1991, Drug Research related to Neuroactive Amino Acids. MunksgaardResearch output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships
Frølund, Bente, Jensen, L. S., Storustovu, S. I., Stensbøl, T. B., Ebert, B., Kehler, J., Krogsgaard-Larsen, Povl & Liljefors, T., 2007, In: Journal of Medicinal Chemistry. 50, 8, p. 1988-1992Research output: Contribution to journal › Journal article › Research › peer-review
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5-(Piperidin-4-yl)-3-Hydroxypyrazole: A Novel Scaffold for Probing the Orthosteric γ-Aminobutyric Acid Type A Receptor Binding Site
Krall, J., Kongstad, Kenneth Thermann, Nielsen, Birgitte, Sørensen, T. E., Balle, T., Jensen, Anders A. & Frølund, Bente, 2014, In: ChemMedChem. 9, 11, p. 2475-2485 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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5-(Piperidine-4-yl)-3-hydroxypyrazole: a novel scaffold forprobing the orthosteric GABAA receptor binding site
Krall, J., Kongstad, Kenneth Thermann, Balle, T., Nielsen, Birgitte, Jensen, A. A. & Frølund, Bente, 2 Sep 2012.Research output: Contribution to conference › Poster › Research
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5-Substituted imidazole-4-acetic acid analogues: Synthesis, modeling, and pharmacological characterization of a series of novel γ-aminobutyric acidC receptor agonists
Madsen, C., Jensen, Anders A., Liljefors, T., Kristiansen, Uffe, Nielsen, Birgitte, Hansen, C. P., Larsen, M., Ebert, B., Bang-Andersen, B., Krogsgaard-Larsen, Povl & Frølund, Bente, 2007, In: Journal of Medicinal Chemistry. 50, p. 4147-4161Research output: Contribution to journal › Journal article › Research › peer-review
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5-substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel ¿-aminobutyric acidC receptor agonists
Madsen, C., Jensen, A. A., Liljefors, T., Kristiansen, Uffe, Nielsen, Birgitte, Hansen, C. P., Larsen, M., Ebert, B., Bang-Andersen, B., Krogsgaard-Larsen, Povl & Frølund, Bente, 2007, In: Journal of Medicinal Chemistry. 50, 17, p. 4147-4161Research output: Contribution to journal › Journal article › Research › peer-review
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7-substituted-melatonin and 7-substituted-1-methylmelatonin analogues: Effect of substituents on potency and binding affinity
Faust, R., Garratt, P. J., Pérez, M. A. T., Piccio, V. J., Madsen, C., Stenstrøm, A., Frølund, Bente, Davidson, K., Teh, M. & Sugden, D., 2007, In: Bioorganic & Medicinal Chemistry. 15, 13, p. 4543-4551Research output: Contribution to journal › Journal article › Research › peer-review
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A CLASS OF SMALL-MOLECULE COMPOUNDS AND THEIR PRODRUGS FOR INTERVENTION WITH CAMK2A, AND THEIR USE IN ACUTE BRAIN INJURIES AND CENTRAL HYPERSOMNIAS
Frølund, Bente, Wellendorph, Petrine & Kornum, Birgitte Rahbek, 2020, Patent No. WO2020151795, 30 Jul 2020, Priority date 21 Jan 2019, Priority No. DK2019PA70040 20190121Research output: Patent
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A Novel Class of Potent 3-Isoxazolol GABAA Antagonists: Design, Synthesis, and Pharmacology
Frølund, Bente, Tagmose, L., Liljefors, T., Stensbøl, T. B., Engblom, C., Kristiansen, Uffe & Krogsgaard-Larsen, Povl, 2000, In: Journal of Medicinal Chemistry. 43, p. 4930–4933Research output: Contribution to journal › Journal article › Research › peer-review
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A novel class of potent 3-isoxazolol GABAA antagonists: Design, systhesis, and pharmacology [3]
Frølund, Bente, Tagmose, L., Liljefors, T., Stensbøl, T. B., Engblom, C., Kristiansen, Uffe & Krogsgaard-Larsen, Povl, 28 Dec 2000, In: Journal of Medicinal Chemistry. 43, 26, p. 4930-4933 4 p.Research output: Contribution to journal › Letter › Research › peer-review
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A novel selective γ-aminobutyric acid transport inhibitor demonstrates a functional role for GABA transporter subtype GAT2/BGT-1 in the CNS
Frølund, Bente, Clausen, Rasmus Prætorius, Larsson, O. M., Schousboe, Arne, Krogsgaard-Larsen, Povl & White, H. S., 2006, In: Neurochemistry International. 48, p. 637–642Research output: Contribution to journal › Journal article › Research › peer-review
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AMPA Receptor Agonists. Synthesis, Protolytic Properties and Pharmacology of 3-Isothiazolol Bioisosteres of Glutamic Acid
Frølund, Bente, Matzen, L., Engesgaard, A., Ebert, B., Didriksen, M., Krogsgaard-Larsen, Povl & Jaroszewski, J., 1997, In: Journal of Medicinal Chemistry. 40, p. 520–527Research output: Contribution to journal › Journal article › Research › peer-review
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Activation of single heteromeric GABAA receptor ion channels by full and partial agonists
Mortensen, M., Kristiansen, Uffe, Ebert, B., Frølund, Bente, Krogsgaard-Larsen, Povl & Smart, T. G., 1 Jun 2004, In: Journal of Physiology. 557, 2, p. 389-413 25 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Activation on single heteromeric GABAA receptor Ion channels by full and partial agonists
Mortensen, M., Kristiansen, Uffe, Ebert, B., Frølund, Bente, Krogsgaard-Larsen, Povl & Smart, T., 2004, In: Journal of Physiology. p. 393–417Research output: Contribution to journal › Journal article › Research › peer-review
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Activity of novel 4-PIOL analogues at human α1β2γ2S GABAAreceptors—correlation with hydrophobicity
Mortensen, M., Frølund, Bente, Jørgensen, A. T., Liljefors, T., Krogsgaard-Larsen, Povl & Ebert, B., 2002, In: European Journal of Medicinal Chemistry. 451, p. 125–132Research output: Contribution to journal › Journal article › Research › peer-review
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Activity of novel 4-PIOL analogues at human α1β2γ2S GABAA receptors - Correlation with hydrophobicity
Mortensen, M., Frølund, Bente, Jorgensen, A. T., Liljefors, T., Krogsgaard-Larsen, Povl & Ebert, B., 13 Sep 2002, In: European Journal of Pharmacology. 451, 2, p. 125-132 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Analogues of the Low-efficacy Partial GABA-A Agonist 4-PIOL. Synthesis and in vitro Pharmacological Studies
De Amici, M., Frølund, Bente, Hjeds, H. & Krogsgaard-Larsen, Povl, 1991, In: European Journal of Medicinal Chemistry. 26, p. 625–631Research output: Contribution to journal › Journal article › Research › peer-review
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Analogues of the low-efficacy partial GABAA agonist 4-PIOL. Syntheses and in vitro pharmacological studies
De Amici, M., Frølund, Bente, Hjeds, H. & Krogsgaard-Larsen, Povl, Sep 1991, In: European Journal of Medicinal Chemistry. 26, 6, p. 625-631 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Astrocytic GABA Transporters: Pharmacological Properties and Targets for Antiepileptic Drugs
Schousboe, Arne, Wellendorph, Petrine, Frølund, Bente, Clausen, Rasmus Prætorius & Krogsgaard-Larsen, Povl, 2017, Glial Amino Acid Transporters. Springer, Vol. 16. p. 283-296 14 p. (Advances in Neurobiology).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Communication
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Autoradiographic imaging and quantification of the high-affinity GHB binding sites in rodent brain using (3)H-HOCPCA
Klein, A. B., Bay, T., Villumsen, I. S., Falk-Petersen, C. B., Marek, A., Frølund, Bente, Clausen, Rasmus Prætorius, Hansen, H. D., Knudsen, Gitte Moos & Wellendorph, Petrine, Nov 2016, In: Neurochemistry International. 100, p. 138-145 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Aza-THIP and Related Analogues of THIP as GABAC Antagonists
Krehan, D., Frølund, Bente, Ebert, B., Nielsen, Birgitte, Krogsgaard-Larsen, Povl, Johnston, G. A. R. & Chebib, M., 2003, In: Bioorganic and Medicinal Chemistry. 11, p. 4891–4896Research output: Contribution to journal › Journal article › Research › peer-review
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Aza-THIP and related analogues of THIP as GABAC antagonists
Krehan, D., Frølund, Bente, Ebert, B., Nielsen, Birgitte, Krogsgaard-Larsen, Povl, Johnston, G. A. R. & Chebib, M., 17 Nov 2003, In: Bioorganic and Medicinal Chemistry. 11, 23, p. 4891-4896 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Bioisosterically Modified Dipeptide Excitatory Amino Acid Receptor Antagonists Containing 3-Oxygenated Isothiazole Ring Systems
Matzen, L., Ebert, B., Stensbøl, T. B., Frølund, Bente, Jaroszewski, J. & Krogsgaard-Larsen, Povl, 1997, In: Bioorganic and Medicinal Chemistry. 5, p. 1569–1575Research output: Contribution to journal › Journal article › Research › peer-review
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CaMK2 modulators and their use in medicine
Frølund, Bente, Shehata, M. A., Wellendorph, Petrine, Gauger, Stine Juul, Kuriyan, J., McSpadden, E. D., Poulsen, Lasse Brokmose, Fougiaxis, V. & Daraj, K., 2023, IPC No. A61K31/4164, A61K31/4178, A61P25/00, C07D277/06, C07D277/12, C07D277/56, C07D417/04, C07D417/10, Patent No. WO2023170024A1, 1 Jan 1970, Priority No. US202263318852PResearch output: Patent
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Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC)
Hansen, C. P., Jensen, Anders A., Balle, T., Bitsch-Jensen, K., Hassan, M. M., Liljefors, T. & Frølund, Bente, 2009, In: Bioorganic & Medicinal Chemistry Letters. 19, 1, p. 87-91Research output: Contribution to journal › Journal article › Research › peer-review
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Carbamoylcholine homologs: synthesis and pharmacology at nicotinic acetylcholine receptors
Jensen, Anders A., Mikkelsen, I. B., Frølund, Bente, Frydenvang, Karla Andrea, Brehm, L., Jaroszewski, J. W., Bräuner, Hans, Falch, E. & Krogsgaard-Larsen, Povl, 2004, In: European Journal of Pharmacology. 497, 2, p. 125-37 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors
Jensen, Anders A., Frølund, Bente, Bräuner, Hans, Falch, E. & Krogsgaard-Larsen, Povl, 2003, In: Molecular Pharmacology. 64, 4, p. 865-75 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Characterization of GABAA receptor ligands in the rat corticalwedge preparation: evidence for action at extrasynaptic receptors?
Ebert, B., Storustovu, S. I., Mortensen, M. S. & Frølund, Bente, 2009, In: British Journal of Pharmacology. 137, 1, p. 1–8Research output: Contribution to journal › Journal article › Research › peer-review
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Characterization of the GABAA Receptor Recognition Site Through Ligand Design and Pharmacophore Modeling
Frølund, Bente, Jørgensen, A. T., Liljefors, T., Mortensen, M. & Krogsgaard-Larsen, Povl, 2004, Molecular Neuropharmacology: Strategies and Methods. Schousboe, A. & Bräuner-Osborne, H. (eds.). Humana PressResearch output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Compounds for the treatment of acute brain injury
Klein, A. B., Leurs, U., Houlton, J., Clausen, Rasmus Prætorius, Frølund, Bente, Clarkson, A. & Wellendorph, Petrine, 2020, Patent No. CN111989094, 24 Nov 2020, Priority date 1 Feb 2019, Priority No. PCT/DK2019/050041Research output: Patent
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Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations
de la Fuente Revenga, M., Balle, T., Jensen, Anders A. & Frølund, Bente, 2015, In: European Journal of Medicinal Chemistry. 102, p. 352-362 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Context-Dependent Modulation of GABAAR-Mediated Tonic Currents
Patel, B., Bright, D. P., Mortensen, M., Frølund, Bente & Smart, T. G., 13 Jan 2016, In: The Journal of neuroscience : the official journal of the Society for Neuroscience. 36, 2, p. 607-21 15 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Correlation between Anticonvulsant Activity and Inhibitory Action on Glial -Aminobutyric Acid Uptake of the Highly Selective Mouse -Aminobutyric Acid Transporter 1 Inhibitor 3-Hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and Its N-Alkylated Analogs
White, S., Sarup, A., Bolvig, T., Petersen, G., Nelson, N., Pickering, Darryl S, Larsson, O. M., Frølund, Bente, Falch, E., Krogsgaard-Larsen, Povl & Schousboe, Arne, 2002, In: Journal of Pharmacology and Experimental Therapeutics. 302, p. 636–644Research output: Contribution to journal › Journal article › Research › peer-review
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Delineation of the functional properties and the mechanism of action of TMPPAA, an allosteric agonist and positive allosteric modulator of 5-HT3 Receptors
Gasiorek, A., Trattnig, S. M., Ahring, P. K., Kristiansen, Uffe, Frølund, Bente, Frederiksen, K. & Jensen, Anders A., 2016, In: Biochemical Pharmacology. 110-111, p. 92-108 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Design and synthesis of a new series of 4-alkylated 3-isoxazolol GABAA antagonists
Frølund, Bente, Tagmose, L., Jørgensen, A. T., Kristiansen, Uffe, Stensbøl, T. B., Liljefors, T. & Krogsgaard-Larsen, Povl, 2003, In: European Journal of Medicinal Chemistry. 38, p. 447–449Research output: Contribution to journal › Journal article › Research › peer-review
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Design and synthesis of a new series of 4-alkylated 3-isoxazolol GABAA antagonists
Frølund, Bente, Tagmose, L., Jørgensen, A. T., Kristiansen, Uffe, Stensbøl, T. B., Liljefors, T. & Krogsgaard-Larsen, Povl, 1 Apr 2003, In: European Journal of Medicinal Chemistry. 38, 4, p. 447-449 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Design, synthesis and pharmacology of model compounds for indirect elucidation of the topography of AMPA receptor sites
Madsen, Ulf, Frølund, Bente, Lund, Trine Meldgaard, Ebert, B. & Krogsgaard-Larsen, Povl, 1993, In: European Journal of Medicinal Chemistry. 28, p. 791–800Research output: Contribution to journal › Journal article › Research › peer-review
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Design, synthesis, and characterisation of selective GABA transport inhibitors
Clausen, Rasmus Prætorius, Moltzen, E., Perregaard, J., Lenz, S., Sanchez, S., Frølund, Bente, Bolvig, T., Sarup, A., Larsson, O., White, H., Schousboe, Arne & Krogsgaard-Larsen, Povl, Aug 2005, In: Journal of Neurochemistry. 94, p. 150-150Research output: Contribution to journal › Conference abstract in journal › Research
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Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites
Sabbatini, P., Wellendorph, Petrine, Høg, S., Pedersen, M. H. F., Bräuner, Hans, Martiny, L., Frølund, Bente & Clausen, Rasmus Prætorius, 2010, In: Journal of Medicinal Chemistry. 53, 17, p. 6506-6510Research output: Contribution to journal › Journal article › Research › peer-review
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Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties
Jensen, Anders A., Plath, N., Pedersen, M. H. F., Isberg, V., Krall, J., Wellendorph, Petrine, Stensbøl, T. B., Gloriam, David E., Krogsgaard-Larsen, Povl & Frølund, Bente, 14 Feb 2013, In: Journal of Medicinal Chemistry. 56, 3, p. 1211-27 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Designing Poly-agonists for Treatment of Metabolic Diseases: Challenges and Opportunities
Petersen, Jonas Odgaard, Strømgaard, Kristian, Frølund, Bente & Clemmensen, Christoffer, 2019, In: Drugs. 79, 11, p. 1187-1197 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Developing New 4-PIOL and 4-PHP Analogues for Photoinactivation of γ-Aminobutyric Acid Type A Receptors
Mortensen, M., Krall, J., Kongstad, Kenneth Thermann, Brygger, B. M., Lenzi, O., Francotte, P., Sørensen, T. E., Nielsen, Birgitte, Jensen, Anders A., Smart, T. G. & Frølund, Bente, 2019, In: ACS Chemical Neuroscience. 10, 11, p. 4669-4684Research output: Contribution to journal › Journal article › Research › peer-review
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Development of Non-GAT1-Selective Inhibitors: Challenges and Achievements
Damgaard, M., Haugaard, A. S., Kickinger, S., Al-Khawaja, A., Lie, M. E. K., Ecker, G. F., Clausen, Rasmus Prætorius & Frølund, Bente, 2017, Advances in Neurobiology. Springer, Vol. 16. p. 315-332 18 p. (Advances in Neurobiology).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Development of a Robust Mammalian Cell-based Assay for Studying Recombinant α4 β1/3 δ GABAA Receptor Subtypes
Falk-Petersen, C. B., Søgaard, R., Madsen, Kenneth Lindegaard, Klein, A. B., Frølund, Bente & Wellendorph, Petrine, Aug 2017, In: Basic & Clinical Pharmacology & Toxicology. 121, 2, p. 119-129 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Differences in kinetics of structurally related competitive GABAA receptor antagonists
Vestergaard, H. T., Cannillo, C., Frølund, Bente & Kristiansen, Uffe, 2007, In: Neuropharmacology. 52, 3, p. 873-882Research output: Contribution to journal › Journal article › Research › peer-review
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Differential effects of two GABA transport inhibitors, tiagabine and EF-1502, on phenytoin-resistant spontaneous bursting in the entorhinal cortex of slices from kainic acid treated rats
Smith-Yockman, M., Saunders, G., Wilcox, K., Clausen, Rasmus Prætorius, Frølund, Bente, Larsson, O., Schousboe, Arne & White, H., 2005, In: Epilepsia. 46, p. 188-188Research output: Contribution to journal › Conference abstract in journal › Research
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Differential interactions of 5-(4-piperidyl)-3-isoxazolol analogues with insect γ-aminobutyric acid receptors leading to functional selectivity
Liu, G., Frølund, Bente, Ozoe, F. & Ozoe, Y., 2015, In: Insect Biochemistry and Molecular Biology. 66, p. 64-71 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery and Evaluation of Anti-Fibrinolytic Plasmin Inhibitors Derived from 5-(4-Piperidyl)isoxazol-3-ol (4-PIOL)
Schmidt, T. C., Eriksson, P., Gustafsson, D., Cosgrove, D., Frølund, Bente & Boström, J., 24 Jul 2017, In: Journal of Chemical Information and Modeling. 57, 7, p. 1703-1714 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1302625
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5-(Piperidine-4-yl)-3-hydroxypyrazole: a novel scaffold forprobing the orthosteric GABAA receptor binding site
Research output: Contribution to conference › Poster › Research
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Functional characterization of GABAA receptor-mediated modulation of cortical neuron network activity in microelectrode array recordings
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Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAA receptors
Research output: Contribution to journal › Journal article › Research › peer-review
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