Bente Frølund
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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Effects of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazol (exo-THPO) and its N-substituted analogs on GABA transport in cultured neurons and astrocytes and by the four cloned mouse GABA transporters
sarup, A., Larsson, O. M., Bolvig, T., Frølund, Bente, Krogsgaard-Larsen, Povl & Schousboe, Arne, 2003, In: Neurochemistry International. 43, p. 445–451Research output: Contribution to journal › Journal article › Research › peer-review
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Muscimol inhibits plasma membrane rupture and ninjurin-1 oligomerization during pyroptosis
den Hartigh, A. B., Loomis, W. P., Anderson, M. J., Frølund, Bente & Fink, S. L., 2023, In: Communications Biology . 6, 1, 1010.Research output: Contribution to journal › Journal article › Research › peer-review
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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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Potentiating action of propofol at GABAA receptors of retinal bipolar cells
Yue, L., Xie, A., Bruzik, K. S., Frølund, Bente, Qian, H. & Pepperberg, D. R., 1 Jan 2011, In: Investigative Ophthalmology & Visual Science. 52, 5, p. 2497-2509Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-Function Evaluation of Imidazopyridine Derivatives Selective for δ-Subunit-Containing γ-Aminobutyric Acid Type A (GABAA) Receptors
Yakoub, K., Jung, S., Sattler, C., Damerow, H., Weber, J., Kretzschmann, A., Cankaya, A. S., Piel, M., Rösch, F., Haugaard, A. S., Frølund, Bente, Schirmeister, T. & Lüddens, H., 8 Mar 2018, In: Journal of Medicinal Chemistry. 61, 5, p. 1951-1968 18 p.Research output: Contribution to journal › Journal article › Research › peer-review
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First Demonstration of a Functional Role for CNS Betaine/GABA Transporter (mGAT2) Based on Synergistic Anticonvulsant Action Among Inhibitors of mGAT1 and mGAT2
White, S., Watson, W. P., Hansen, S. L., Slough, S., Perregård, J., Sarup, A., Bolvig, T., Petersen, G., Larsson, O. M., Clausen, Rasmus Prætorius, Frølund, Bente, Falch, E., Krogsgaard-Larsen, Povl & Schousboe, Arne, 2005, In: The Journal of Pharmacology and Experimental Therapeutics. 312, p. 866–874Research 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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Novel radioiodinated γ-hydroxybutyric acid analogues for radiolabeling and photolinking of high-affinity γ-hydroxybutyric acid binding sites
Wellendorph, Petrine, Høg, S., Sabbatini, P., Pedersen, M. H. F., Martiny, L., Knudsen, Gitte Moos, Frølund, Bente, Clausen, Rasmus Prætorius & Bräuner, Hans, 2010, In: Journal of Pharmacology and Experimental Therapeutics. 335, 2, p. 458-464Research output: Contribution to journal › Journal article › Research › peer-review
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Novel cyclic gamma-hydroxybutyrate (GHB) analogs with high affinity and stereoselectivity of binding to GHB sites in rat brain
Wellendorph, Petrine, Høg, S., Greenwood, J. R., de Lichtenberg, A., Nielsen, Birgitte, Frølund, Bente, Brehm, L., Clausen, Rasmus Prætorius & Bräuner, Hans, Oct 2005, In: Journal of Pharmacology and Experimental Therapeutics. 315, 1, p. 346-51Research output: Contribution to journal › Journal article › Research › peer-review
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TREATMENT OF CNS DISORDERS WITH SLEEP DISTURBANCES
Wellendorph, Petrine, Kornum, Birgitte Rahbek & Frølund, Bente, 2020, Patent No. WO2020259787 , 30 Dec 2020, Priority date 28 Jun 2019, Priority No. DK2019PA70415 20190628Research output: Patent
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New synthesis and tritium labeling of a selective ligand for studying high-affinity γ-hydroxybutyrate (GHB) binding sites
Vogensen, S. B., Marek, A., Bay, T., Wellendorph, Petrine, Kehler, J., Bundgaard, C., Frølund, Bente, Pedersen, M. H. F. & Clausen, Rasmus Prætorius, 2013, In: Journal of Medicinal Chemistry. 56, 20, p. 8201–8205Research output: Contribution to journal › Journal article › Research › peer-review
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Målrettet fisketur i hjernen giver ny viden om Fantasy’s virkningssted
Villumsen, I. S., Vogensen, S. B., Frølund, Bente, Clausen, Rasmus Prætorius & Wellendorph, Petrine, 2011, In: Lægemiddelforskning. 2011, p. 26-28Research output: Contribution to journal › Journal article › Communication
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Målrettet fisketur i hjernen giver ny viden om Fantasys virkningssted
Villumsen, I. S., Vogensen, S. B., Frølund, Bente, Clausen, Rasmus Prætorius & Wellendorph, Petrine, Dec 2011, In: Lægemiddelforskning. 2011, p. 26-28Research output: Contribution to journal › Journal article › Communication
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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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Imidazole-4-acetic acid, a new lead structure for interaction with the taurine transporter in outer blood-retinal barrier cells
Valembois, S. A. N., Krall, J., Frølund, Bente & Steffansen, B., 30 May 2017, In: European Journal of Pharmaceutical Sciences. 103, p. 77-84 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis, pharmacology and biostructural characterization of novel a4ß2 nicotinic acetylcholine receptor agonists
Ussing, C. A., Hansen, C. P., Petersen, J. G., Jensen, Anders A., Rohde, L. A. H., Ahring, P. K., Nielsen, E. Ø., Kastrup, Jette Sandholm Jensen, Gajhede, Michael, Frølund, Bente & Balle, T., 2013, In: Journal of Medicinal Chemistry. 56, 3, p. 940-951Research output: Contribution to journal › Journal article › Research › peer-review
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Exploring the NCS-382 Scaffold for CaMKII alpha Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKII alpha Hub Domain
Tian, Yongsong, Shehata, M. A., Gauger, Stine Juul, Veronesi, C., Hamborg, L., Thiesen, L., Bruus-Jensen, J., Royssen, J. S., Leurs, U., Larsen, A. S. G., Krall, J., Solbak, Sara Marie Øie, Wellendorph, Petrine & Frølund, Bente, 2022, In: Journal of Medicinal Chemistry. 65, 22, p. 15066–15084Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery and Optimization of 5-Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain
Tian, Yongsong, Shehata, M. A., Gauger, Stine Juul, Ng, C. K. L., Solbak, Sara Marie Øie, Thiesen, L., Bruus-Jensen, J., Krall, J., Bundgaard, C., Gibson, K. M., Wellendorph, Petrine & Frølund, Bente, 2022, In: Journal of Medicinal Chemistry. 65, 9, p. 6656-6676Research output: Contribution to journal › Journal article › Research › peer-review
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Lack of evidence for synaptic high-affinity γ-hydroxybutyric acid (GHB) transport in rat brain synaptosomes and 11 Na+ -dependent SLC neurotransmitter transporters
Thiesen, L., Frølund, Bente & Wellendorph, Petrine, Apr 2019, In: Journal of Neurochemistry. 149, 2, p. 195-210 16 p.Research output: Contribution to journal › Journal article › Research › peer-review
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In vitro and in vivo evidence for active brain uptake of the GHB analogue HOCPCA by the monocarboxylate transporter subtype 1
Thiesen, L., Kehler, J., Clausen, Rasmus Prætorius, Frølund, Bente, Bundgaard, C. & Wellendorph, Petrine, 2015, In: Journal of Pharmacology and Experimental Therapeutics. 354, 2, p. 166-174 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Effect of tiagabine and EF1502 on phenytoin-resistant spontaneous bursts in the entorhinal cortex of slices from kainic acid-treated rats
Smith-Yockman, M., Saunders, G., Wilcox, K., Larsson, O., Clausen, Rasmus Prætorius, Frølund, Bente, Schousboe, Arne & White, H., Aug 2005, In: Journal of Neurochemistry. 94, p. 256-256Research output: Contribution to journal › Conference abstract in journal › Research
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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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Inhibition of the betaine-GABA transporter (mGAT2/BGT-1) modulates spontaneous electrographic bursting in the medial entorhinal cortex (mEC)
Smith, M. D., Saunders, G. W., Clausen, Rasmus Prætorius, Frølund, Bente, Krogsgaard-Larsen, Povl, Larsson, O. M., Schousboe, Arne, Wilcox, K. S. & White, H. S., 2008, In: Epilepsy Research. 79, 1, p. 6-13Research 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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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
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New insights into the GABAA receptor structure and orthosteric ligand binding: Receptor modeling guided by experimental data
Sander, T., Frølund, Bente, Bruun, A. T., Ivanov, I., McCammon, J. A. & Balle, T., May 2011, In: Proteins: Structure, Function, and Bioinformatics. 79, 5, p. 1458-1477Research output: Contribution to journal › Journal article › Research › peer-review
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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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Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors
Rostrup, F., Falk-petersen, C. B., Harpsøe, Kasper, Buchleithner, S., Conforti, I., Jung, S., Gloriam, David E., Schirmeister, T., Wellendorph, Petrine & Frølund, Bente, 22 Apr 2021, In: Journal of Medicinal Chemistry. 64, 8, p. 4730-4743 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Substituted 4-hydroxy-1,2,3-triazoles: synthesis, characterization and first drug design applications through bioisosteric modulation and scaffold hopping approaches
Pippione, A. C., Dosio, F., Ducime, A., Federico, A., Martina, K., Sainas, S., Frølund, Bente, Gooyit, M., Janda, K. D., Boschi, D. & Lolli, M. L., 1 Jul 2015, In: MedChemComm. 6, 7, p. 1285-1292 8 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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Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as ¿-aminobutyric acidA receptor agonists
Petersen, J. G., Bergmann, R., Møller, H. A., Jørgensen, Charlotte Grube, Nielsen, Birgitte, Kehler, J., Frydenvang, Karla Andrea, Kristensen, Jesper Langgaard, Balle, T., Jensen, Anders A., Kristiansen, Uffe & Frølund, Bente, 2013, In: Journal of Medicinal Chemistry. 56, 3, p. 993-1006Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel γ-aminobutyric acidA receptor agonists
Petersen, J. G., Sørensen, T. E., Damgaard, M., Nielsen, Birgitte, Jensen, Anders A., Balle, T., Bergmann, R. & Frølund, Bente, 2014, In: European Journal of Medicinal Chemistry. 84, p. 404-416 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Probing the orthosteric binding site of GABAA receptors with heterocyclic GABA carboxylic acid bioisosteres
Petersen, J. G., Bergmann, R., Krogsgaard-Larsen, Povl, Balle, T. & Frølund, Bente, 21 Dec 2013, In: Neurochemical Research. 39, p. 1005-1015Research 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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Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acidA receptor ligands: synthesis, pharmacology, and structure-activity relationships
Møller, H. A., Sander, T., Kristensen, Jesper Langgaard, Nielsen, Birgitte, Krall, J., Bergmann, M. L., Christiansen, B., Balle, T., Jensen, Anders A. & Frølund, Bente, 2010, In: Journal of Medicinal Chemistry. 53, 8, p. 3417-3421Research 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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Pregnenolone sulfate analogues differentially modulate GABAA receptor closed/desensitised states
Mortensen, M., Xu, Y., Shehata, M. A., Krall, J., Ernst, M., Frølund, Bente & Smart, T. G., 2023, In: British Journal of Pharmacology. 180, 19, p. 2482-2499Research 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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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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Erratum: Activity of novel 4-PIOL analogues at human α1β2γ2S GABAA receptors - Correlation with hydrophobicity (European Journal of Pharmacology (2000) 451 (125-132))
Mortensen, M., Frølund, Bente, Jorgensen, A. T., Liljefors, T., Krogsgaard-Larsen, Povl & Ebert, B., 25 Oct 2002, In: European Journal of Pharmacology. 453, 2-3, p. 345-346 2 p.Research output: Contribution to journal › Comment/debate › 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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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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The labeling of unsaturated γ-hydroxybutyric acid by heavy isotopes of hydrogen: iridium complex-mediated H/D exchange by C─H bond activation vs reduction by boro-deuterides/tritides
Marek, A., Pedersen, M. H. F., Vogensen, S. B., Clausen, Rasmus Prætorius, Frølund, Bente & Elbert, T., Oct 2016, In: Journal of Labelled Compounds and Radiopharmaceuticals. 59, 12, p. 476-483 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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GABA and Glutamate Receptor Ligands and Therapeutic Potential in CNS Disorders
Madsen, Ulf, Greenwood, J., Johansen, Tommy Nørskov, Krogsgaard-Larsen, Povl, Liljefors, T., Nielsen, M. & Frølund, Bente, 2005, Drug Discovery Handbook. Wiley, p. 797–907Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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GABA and Glutamate Receptor Ligands and Their Therapeutic Potential in CNS Disorders
Madsen, Ulf, Bräuner, Hans, Greenwood, J. R., Johansen, Tommy Nørskov, Krogsgaard-Larsen, Povl, Liljefors, T., Nielsen, M. & Frølund, Bente, 27 Jan 2005, Drug Discovery Handbook. John Wiley & Sons, Inc., p. 797-907 111 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › 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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Functional and Pharmacological Aspects of GABA Transporters
Madsen, K., White, S. H., Clausen, Rasmus Prætorius, Larsson, O. M., Frølund, Bente, Krogsgaard-Larsen, Povl & Schousboe, Arne, 2006, Handbook of Neurochemistry and Molecular neurobiology. p. 1-17Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Functional and pharmacological aspects of GABA transporters
Madsen, K., White, H. S., Clausen, Rasmus Prætorius, Frølund, Bente, Larsson, O. M., Krogsgaard-Larsen, Povl & Schousboe, Arne, 2007, Handbook of nerochemistry and molecular neurobiology: Neural membranes and transport. Lajtha, A. & Reith, M. E. A. (eds.). 3rd. ed. Berlin: Springer, Vol. 3. p. 285-304Research output: Chapter in Book/Report/Conference proceeding › Book chapter › 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-(Piperidine-4-yl)-3-hydroxypyrazole: a novel scaffold forprobing the orthosteric GABAA receptor binding site
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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
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