Bente Frølund
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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α4βδ GABA receptors are high-affinity targets for γ-hydroxybutyric acid (GHB)
Absalom, N., Karim, N., Eghorn, L. F., Villumsen, I. S., Bay, T., Bräuner, Hans, Frølund, Bente, Clausen, Rasmus Prætorius, Olsen, Jesper Velgaard, Knudsen, Gitte Moos, Chebib, M. & Wellendorph, Petrine, 14 Aug 2012, In: Proceedings of the National Academy of Sciences USA (PNAS). 109, 33, p. 13404-13409 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological Characterization of [3H]ATPCA as a Substrate for Studying the Functional Role of the Betaine/GABA Transporter 1 and the Creatine Transporter
Al-Khawaja, A., Haugaard, A. S., Marek, A., Löffler, R., Thiesen, L., Santiveri, M., Damgaard, M., Bundgaard, C., Frølund, Bente & Wellendorph, Petrine, 21 Mar 2018, In: A C S Chemical Neuroscience. 9, 3, p. 545–554Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological Identification of a Guanidine-Containing β-Alanine Analogue with Low Micromolar Potency and Selectivity for the Betaine/GABA Transporter 1 (BGT1)
Al-Khawaja, A. M. A., Petersen, J. G., Damgaard, M., Jensen, M. H., Vogensen, S. B., Lie, M. E. K., Kragholm, B., Bräuner, Hans, Clausen, Rasmus Prætorius, Frølund, Bente & Wellendorph, Petrine, 23 May 2014, In: Neurochemical Research. 39, 10, p. 1988-1996 9 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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Exploration of the molecular architecture of the orthosteric binding site in the α4β2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.
Bach, T. B., Jensen, Anders A., Petersen, J. G., Sørensen, T. E., Volpe, S. D., Liu, J., Blaazer, A. R., van Muijlwijk-Koezen, J. E., Balle, T. & Frølund, Bente, 2015, In: European Journal of Medicinal Chemistry. 102, p. 425-444 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Functional characterization of GABAA receptor-mediated modulation of cortical neuron network activity in microelectrode array recordings
Bader, B. M., Steder, A., Klein, A. B., Frølund, Bente, Schroeder, O. H. U. & Jensen, Anders A., 2017, In: PloS One. 12, 10, 32 p., e0186147.Research output: Contribution to journal › Journal article › Research › peer-review
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Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine
Bavo, Francesco, Kickinger, Stefanie, Lie, M. E. K., Avgerinos, Christos, Wilhelmsen, Kristine Sloth, Wellendorph, Petrine & Frølund, Bente, 2023, In: Medicinal Chemistry Research. 32, p. 2299–2324Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based ?-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect
Bavo, Francesco, De-Jong, H., Petersen, Jonas Odgaard, Falk-Petersen, C. B., Löffler, R., Sparrow, E., Rostrup, F., Eliasen, Jannik Nicklas, Wilhelmsen, K. S., Barslund, K., Bundgaard, C., Nielsen, Birgitte, Kristiansen, Uffe, Wellendorph, Petrine, Bogdanov, Y. & Frølund, Bente, 2021, In: Journal of Medicinal Chemistry. 64, 24, p. 17795-17812Research output: Contribution to journal › Journal article › Research › peer-review
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The GABAA Antagonist DPP-4-PIOL Selectively Antagonises Tonic over Phasic GABAergic Currents in Dentate Gyrus Granule Cells
Boddum, K., Frølund, Bente & Kristiansen, Uffe, 8 Aug 2014, In: Neurochemical Research. 39, 11, p. 2078–2084 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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The human proton-coupled amino acid transporter (hPAT1) is a transport system for GABA-like drugs
Broberg, M. L., Frølund, Bente, Larsen, Birger Brodin & Nielsen, C. U., 2007. 1 p.Research output: Contribution to conference › Conference abstract for conference › Research › peer-review
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Incorporation of the crossfire Beilstein database into the organic chemistry curriculum at the Royal Danish School of Pharmacy
Christensen, Søren Brøgger, Franzyk, Henrik, Frølund, Bente, Jaroszewski, J. W., Stærk, Dan & Vedsø, P., 1 Jun 2002, In: Journal of Chemical Education. 79, 6, 1 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Incorporation of the Cross Fire Beilstein database in the organic chemistry curriculum at the Royal Danish School of Pharmacy
Christensen, Søren Brøgger, Franzyk, Henrik, Frølund, Bente, Jaroszewski, J. W., Stærk, Dan & Vedsø, P., 2002, In: Journal of Chemical Education. 79, p. 765-768Research output: Contribution to journal › Journal article › Research
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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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Structure-Activity Relationship and Pharmacology of γ-Aminobutyric Acid (GABA) Transport Inhibitors
Clausen, Rasmus Prætorius, Madsen, K., Larsson, O. M., Frølund, Bente, Krogsgaard-Larsen, Povl & Schousboe, Arne, 1 Dec 2006, GABA. Enna, S. J. (ed.). p. 265-284 20 p. (Advances in Pharmacology, Vol. 54).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Selective inhibitors of GABA uptake: synthesis and molecular pharmacology of 4-N-methylamino- 4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol analogues
Clausen, Rasmus Prætorius, Moltzen, E. K., Perregaard, J., Lenz, S., Sanchez, C., Falch, E., Frølund, Bente, Bolvig, T., Sarup, A., Larsson, O. M., Schousboe, Arne & Krogsgaard-Larsen, Povl, 2005, In: Bioorganic & Medicinal Chemistry. 13, p. 895–908Research output: Contribution to journal › Journal article › Research › peer-review
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Structure–Activity Relationship and Pharmacology of γ‐Aminobutyric Acid Transport Inhibitor
Clausen, Rasmus Prætorius, Madsen, K., Larsson, O. M., Frølund, Bente, Krogsgaard-Larsen, Povl & Schousboe, Arne, 2006, GABA. Enna, S. (ed.). Vol. 54. p. 265–284 (Advances in Pharmacology).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Synthesis of 3-Hydroxy- and 3-Carboxy-Δ2-isoxazoline Amino Acids and Evaluation of Their Interaction with GABA Receptors and Transporters
Conti, P., De Amici, M., Pinto, A., Tamborini, L., Grazioso, G., Frølund, Bente, Nielsen, Birgitte, Thomsen, C., Ebert, B. & De Michelli, C., 2006, In: European Journal of Pharmacology. p. 5533–5542Research output: Contribution to journal › Journal article › Research › peer-review
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Silencing of spontaneous activity at α4β1/3δ GABAA receptors in hippocampal granule cells reveals different ligand pharmacology
Dalby, N. O., Falk-Petersen, C. B., Leurs, U., Scholze, P., Krall, J., Frølund, Bente & Wellendorph, Petrine, 2020, In: British Journal of Pharmacology. 177, 17, p. 3975-3990Research output: Contribution to journal › Journal article › Research › peer-review
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Monastrol, a 3,4-dihydropyrimidin-2(1H)-thione, as structural scaffold for the development of modulators for GHB high-affinity binding sites and α1β2δ GABAA receptors
Damgaard, M., Al-Khawaja, A., Nittegaard-Nielsen, M., Petersen, R. F., Wellendorph, Petrine & Frølund, Bente, 15 Jun 2017, In: European Journal of Medicinal Chemistry. 138, p. 300-312 13 p.Research 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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Identification of the first highly selective inhibitor of human GABA transporter GAT3
Damgaard, M., Al-Khawaja, A., Vogensen, S. B., Jurik, A., Sijm, M., Lie, M., Bæk, M. I., Rosenthal, E., Jensen, Anders A., Ecker, G. F., Frølund, Bente, Wellendorph, Petrine & Clausen, Rasmus Prætorius, 2015, In: A C S Chemical Neuroscience. 6, p. 1591-1599 9 p.Research 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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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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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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Equilibrium binding characteristics of [3H]thiomuscimol
Ebert, B., Frølund, Bente, Diemer, N. & Krogsgaard-Larsen, Povl, 1999, In: Neurochemistry International. 34, p. 427–434Research output: Contribution to journal › Journal article › Research › peer-review
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Positive allosteric modulation of the GHB high-affinity binding site by the GABAA receptor modulator monastrol and the flavonoid catechin
Eghorn, L. F., Høstgaard-Jensen, K., Kongstad, Kenneth Thermann, Bay, T., Higgins, D., Frølund, Bente & Wellendorph, Petrine, 5 Oct 2014, In: European Journal of Pharmacology. 740, p. 570-577 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Sex-specific alterations in GABA receptor-mediated responses in laterodorsal tegmentum (LDT) are associated with prenatal exposure to nicotine
Eliasen, Jannik Nicklas, Krall, J., Frølund, Bente & Kohlmeier, Kristi Anne, 2020, In: Developmental Neurobiology. 80, 5-6, p. 178-199Research output: Contribution to journal › Journal article › Research › peer-review
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Selective Inhibitors of Glial GABA Uptake: Synthesis, Absolute Stereochemistry, and Pharmacology of the Enantiomers of 3-Hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole (exo-THPO) and Analogues
Falch, E., Frølund, Bente, Perregaard, Sanchez, C., Søkilde, B., Buur, A., Hansen, A., Frydenvang, Karla Andrea, Brehm, L., Bolvig, T., Larsson, O. M., Schousboe, Arne & Krogsgaard-Larsen, Povl, 1999, In: Journal of Medicinal Chemistry. 42, p. 5402–5414Research output: Contribution to journal › Journal article › 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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Molecular Determinants underlying Delta Selective Compound 2 (DS2) Activity at δ-Containing GABAA Receptors
Falk-Petersen, C. B., Rostrup, F., Löffler, R., Buchleihtner, S., Harpsøe, Kasper, Gloriam, David E., Frølund, Bente & Wellendorph, Petrine, 2021, In: Molecular Pharmacology. 100, 1, p. 46-56Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAA receptors
Falk-Petersen, C. B., Tsonkov, T. M., Nielsen, M. S., Harpsøe, Kasper, Bundgaard, C., Frølund, Bente, Kristiansen, Uffe, Gloriam, David E. & Wellendorph, Petrine, 22 Jun 2020, In: Scientific Reports. 10, 1, 12 p., 10078.Research 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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Stereospecific GABA-B receptor antagonism
Frydenvang, Karla Andrea, Frølund, Bente, Kristiansen, Uffe & Krogsgaard-Larsen, Povl, 1996, GABA, receptors, transporters and metabolism. Tanaka, C. & Bowery, N. G. (eds.). Basel: Birkhäuser VerlagResearch output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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GABA-B Antagonists: Enantiopharmacology of 5-Amino-4-hydroxy-2-methylvaleric Acid and X-Ray Structure of the Eutomer
Frydenvang, Karla Andrea, Kristiansen, Uffe, Frølund, Bente, Herdeis, C. & Krogsgaard-Larsen, Povl, 1995, In: Chirality. 7, p. 526–533Research 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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Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABAA antagonists: Synthesis, pharmacology, and molecular modeling
Frølund, Bente, Jensen, L. S., Guandalini, L., Canillo, C., Vestergaard, H. T., Kristiansen, Uffe, Nielsen, Birgitte, Stensbøl, T. B., Madsen, C., Krogsgaard-Larsen, Povl & Liljefors, T., 27 Jan 2005, In: Journal of Medicinal Chemistry. 48, 2, p. 427-439 13 p.Research output: Contribution to journal › Journal article › 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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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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GABAA Agonists: Resolution and Pharmacology of (+)- and (-)-Isoguvacine Oxide
Frølund, Bente, Jeppesen, L., Krogsgaard-Larsen, Povl & Hansen, J. J., 1995, In: Chirality. 7, p. 434–438Research 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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Partial GABAA Receptor agonists. Synthesis and in vitro Pharmacology
Frølund, Bente, Kristiansen, Uffe, Brehm, L., Hansen, A. B., Krogsgaard-Larsen, Povl & Falch, E., 1995, In: Journal of Medicinal Chemistry. 38, p. 3287–3296Research output: Contribution to journal › Journal article › Research › peer-review
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GABA(A) receptor ligands and their therapeutic potentials.
Frølund, Bente, Ebert, B., Kristiansen, Uffe, Liljefors, T. & Krogsgaard-Larsen, Povl, Aug 2002, In: Current Topics in Medicinal Chemistry. 2, 8, p. 817-832 16 p.Research output: Contribution to journal › Review › 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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Phosphinic, phosphonic and seleninic acid bioisosteres of isonipecotic acid as novel and selective GABAC receptor antagonists
Frølund, Bente, Krehan, D., Krogsgaard-Larsen, Povl, Kehler, J., Johnston, G. A. R. & Chebib, M., 2003, In: Neurochemistry International. 42, p. 561–565Research output: Contribution to journal › Journal article › Research › peer-review
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Potent 4-Aryl- or 4-Arylalkyl-Substituted 3-Isoxazolol GABAA Antagonists: Synthesis, Pharmacology, and Molecular Modeling
Frølund, Bente, Jensen, L. S., Guandalini, L., Canillo, C., Vestergaard, H. T., Kristiansen, U., Nielsen, Birgitte, Stensbøl, T. B., Madsen, C., Krogsgaard-Larsen, Povl & Liljefors, T., 2005, In: Journal of Medicinal Chemistry. 48, p. 427–439Research output: Contribution to journal › Journal article › Research › peer-review
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Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABAA antagonists: Synthesis, pharmacology, and molecular modeling
Frølund, Bente, Jørgensen, A. T., Tagmose, L., Stensbøl, T. B., Vestergaard, H. T., Engblom, C., Kristiansen, Uffe, Sanchez, C., Krogsgaard-Larsen, Povl & Liljefors, T., 6 Jun 2002, In: Journal of Medicinal Chemistry. 45, 12, p. 2454-2468 15 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and receptor binding of 5-amino[3H]2methyl-3-isothiazolol ([3H]thiomuscimol), a specific GABAa agonist photoaffinity label
Frølund, Bente, Ebert, B., Lawrence, L. W., Hurt, S. D. & Krogsgaard-Larsen, Povl, 1995, In: Journal of Labelled Compounds and Radiopharmaceuticals. 36, p. 877–889Research output: Contribution to journal › Journal article › Research › peer-review
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Tetrazolyl isoxazole amino acids as ionotropic glutamate receptor antagonists: synthesis, modelling and molecular pharmacology
Frølund, Bente, Greenwood, J. R., Holm, M. M., Egebjerg, J., Madsen, Ulf, Nielsen, Birgitte, Bräuner, Hans, Stensbøl, T. B. & Krogsgaard-Larsen, Povl, 15 Sep 2005, In: Bioorganic & Medicinal Chemistry. 13, 18, p. 5391-8Research output: Contribution to journal › Journal article › Research › peer-review
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Effekt og bivirkninger: GABA fra A til C.
Frølund, Bente, Madsen, C., Jensen, Anders A., Kristiansen, Uffe & Liljefors, T., 2006, In: Lægemiddelforskning. p. 32-33Research output: Contribution to journal › Journal article › Communication
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
Research output: Contribution to journal › Journal article › Research › peer-review
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181
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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
Published