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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GABAA agonists: Resolution and pharmacology of (+)‐ and (−)‐isoguvacine oxide
Frølund, Bente, Jeppesen, L., Krogsgaard-Larsen, Povl & Hansen, J. J., 1995, In: Chirality. 7, 6, p. 434-438 5 p.Research 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., 2002, In: Journal of Medicinal Chemistry. 45, p. 2454–2468Research output: Contribution to journal › Journal article › Research › peer-review
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GABA-A Receptor Agonists, Partial Agonists and Antagonists
Frølund, Bente, Krogsgaard-Larsen, Povl & Ebert, B., 1996, The GABA Receptors. 2nd ed. Humana PressResearch output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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GABAA receptor ligands and their therapeutic potentials
Frølund, Bente, Ebert, B., Kristiansen, Uffe, Liljefors, T. & Krogsgaard-Larsen, Povl, 2002, In: Current Topics in Medicinal Chemistry. 2Research output: Contribution to journal › Journal article › Research › peer-review
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Partial GABAA Receptor Agonists. Synthesis and in Vitro Pharmacology of a Series of Nonannulated Analogs of 4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3-ol
Frølund, Bente, Kristiansen, Uffe, Brehm, L., Hansen, A. B., Krogsgaard-Larsen, Povl & Falch, E., 1 Aug 1995, In: Journal of Medicinal Chemistry. 38, 17, p. 3287-3296 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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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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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GABA-A and GABA-B receptor Agonists, Partial Agonists and Modulators. design and Therapeutic Prospects
Frølund, Bente, Krogsgaard-Larsen, Povl, Kristiansen, Uffe, Frydenvang, Karla Andrea & Ebert, B., 1997, In: European Journal of Pharmaceutical Sciences. 4, p. 355–384Research 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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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 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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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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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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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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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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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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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
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GABA and glutamic acid receptor ligands
Frølund, Bente & Madsen, Ulf, 2010, Textbook of drug design and discovery. Krogsgaard-Larsen, P., Strømgaard, K. & Madsen, U. (eds.). 4 ed. Boca Raton: CRC Press, p. 239-262Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
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GABAA-receptoren: Bedre modeller - bedre lægemidler
Frølund, Bente, Sander, T., Hansen, H. & Balle, T., 2009, In: Lægemiddelforskning. p. 31-33Research output: Contribution to journal › Journal article › Communication
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Ligands for the GABA recognition site at the GABAA receptor: Structure-activity studies
Frølund, Bente, Kristiansen, Uffe, Krogsgaard-Larsen, Povl & Liljefors, T., 2008, Chemistry and molecular aspects of drug design and action. Rekka, E. A. & Kourounakis, P. N. (eds.). Boca Raton, Fl: CRC Press, p. 139-147Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research
- Published
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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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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Five-membered N-heterocyclic Scaffolds as Novel Amino Bioisosteres at gamma-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters
Giraudo, A., Krall, J., Bavo, Francesco, Nielsen, Birgitte, Kongstad, Kenneth Thermann, Rolando, B., De Blasio, R., Gloriam, David E., Löffler, R., Thiesen, L., Harpsøe, Kasper, Frydenvang, Karla Andrea, Boschi, D., Wellendorph, Petrine, Lolli, M. L., Jensen, Anders A. & Frølund, Bente, 27 Jun 2019, In: Journal of Medicinal Chemistry. 62, 12, p. 5797-5809Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology
Griem-Krey, Nane, Frølund, Bente, Marek, A. & Wellendorph, Petrine, 2021, In: Journal of Labelled Compounds and Radiopharmaceuticals. 64, 2, 77 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
The CaMKIIα hub ligand Ph-HTBA promotes neuroprotection after focal ischemic stroke by a distinct molecular interaction
Griem-Krey, Nane, Gauger, Stine Juul, Gowing, E. K., Thiesen, L., Frølund, Bente, Clarkson, A. N. & Wellendorph, Petrine, 2022, In: Biomedicine and Pharmacotherapy. 156, 10 p., 113895.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Novel acetylcholine and carbamoylcholine analogues: Development of a functionally selective a4ß2 nicotinic acetylcholine receptor agonist
Hansen, C. P., Jensen, Anders A., Christensen, J. K., Balle, T., Liljefors, T. & Frølund, Bente, 2008, In: Journal of Medicinal Chemistry. 51, 23, p. 7380-7395Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
GABAergic control of arteriolar diameter in the rat retina
Hinds, K., Monaghan, K. P., Frølund, Bente, McGeown, J. G. & Curtis, T. M., 2013, In: Invest. Ophthalmol. Vis. Sci.. 54, 10, p. 6798–6805Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
The orthosteric GABAA receptor ligand Thio-4-PIOL displays distinctly different functional properties at synaptic and extrasynaptic receptors
Hoestgaard-Jensen, K., O'Connor, R. M., Dalby, N. O., Simonsen, C., Finger, B. C., Golubeva, A., Hammer, H., Bergmann, M. L., Kristiansen, Uffe, Krogsgaard-Larsen, Povl, Bräuner, Hans, Ebert, B., Frølund, Bente, Cryan, J. F. & Jensen, Anders A., Oct 2013, In: British Journal of Pharmacology. 170, 4, p. 919-32 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Probing α4βδ GABAA Receptor Heterogeneity: Differential Regional Effects of a Functionally Selective α4β1δ/α4β3δ Receptor Agonist on Tonic and Phasic Inhibition in Rat Brain
Hoestgaard-Jensen, K., Dalby, N. O., Krall, J., Hammer, H., Krogsgaard-Larsen, Povl, Frølund, Bente & Jensen, Anders A., 2014, In: Journal of Neuroscience. 34, 49, p. 16256-16272 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
MEDI 480-Novel lipophilic gamma-hydroxybutyrate (GHB) analogs with high affinity to GHB sites in rat brain
Hog, S., Wellendorph, Petrine, Nielsen, Birgitte, Frølund, Bente & Clausen, Rasmus Prætorius, 10 Sep 2006, In: American Chemical Society. Abstracts of Papers (at the National Meeting). 232Research output: Contribution to journal › Conference abstract in journal › Research
- Published
Structure-Activity Relationships of Selective GABA Uptake Inhibitors
Høg, S., Greenwood, J., Madsen, K. B., Larsson, O. M., Frølund, Bente, Schousboe, Arne, Krogsgaard-Larsen, Povl & Clausen, Rasmus Prætorius, 2006, In: Current Topics in Medicinal Chemistry. 6, 17, p. 1861–1882Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Novel high-affinity and selective biaromatic 4-substituted ¿-hydroxybutyric acid (GHB) analogues as GHB ligands: design, synthesis, and binding studies
Høg, S., Wellendorph, Petrine, Nielsen, Birgitte, Frydenvang, Karla Andrea, Dahl, I. F., Bräuner, Hans, Brehm, L., Frølund, Bente & Clausen, Rasmus Prætorius, 2008, In: Journal of Medicinal Chemistry. 51, 24, p. 8088-8095Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Neuroactive Polyamine Wasp Toxins: Nuclear Magnetic Resonance Spectroscopic Analysis of the Proteolytic Properties of Philantotoxin-343
Jaroszewski, J., Matzen, L., Frølund, Bente & Krogsgaard-Larsen, Povl, 1996, In: Journal of Medicinal Chemistry. 39, p. 515–521Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Neuroactive polyamine wasp toxins: Nuclear magnetic resonance spectroscopic analysis of the protolytic properties of philanthotoxin-343
Jaroszewski, J. W., Matzen, L., Frølund, Bente & Krogsgaard-Larsen, Povl, 19 Jan 1996, In: Journal of Medicinal Chemistry. 39, 2, p. 515-521 7 p.Research 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
- Published
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
- Published
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
- Published
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations
Jensen, Anders A., Frølund, Bente, Liljefors, T. & Krogsgaard-Larsen, Povl, 2005, In: Journal of Medicinal Chemistry. 48, 15, p. 4705-45 41 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites
Jensen, C. H., Hansen, H. D., Bay, T., Vogensen, S. B., Lehel, S., Thiesen, L., Bundgaard, C., Clausen, Rasmus Prætorius, Knudsen, Gitte Moos, Herth, Matthias Manfred, Wellendorph, Petrine & Frølund, Bente, 18 Jan 2017, In: A C S Chemical Neuroscience. 8, 1, p. 22-27 6 p.Research output: Contribution to journal › Letter › Research › peer-review
- Published
Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists
Jørgensen, Charlotte Grube, Frølund, Bente, Kehler, J. & Jensen, Anders A., 4 Apr 2011, In: ChemMedChem. 6, 4, p. 725-736Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Exploring the molecular determinants for subtype-selectivity of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogs as betaine/GABA transporter 1 (BGT1) substrate-inhibitors
Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Lie, M. E. K., Bavo, Francesco, Loeffler, R., Damgaard, M., Ecker, G. F., Frølund, Bente & Wellendorph, Petrine, 2020, In: Scientific Reports. 10, 1, 15 p., 12992.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Synthesis, pharmacological activity and molecular modeling studies of a series of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogues as betaine/GABA transporter 1 (BGT1) substrate-inhibitors
Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Loeffler, R., Damgaard, M., Eckert, G., Frølund, Bente & Wellendorph, Petrine, 19 Aug 2018.Research output: Contribution to conference › Conference abstract for conference › Research › peer-review
- Published
Molecular Determinants and Pharmacological Analysis for a Class of Competitive Non-transported Bicyclic Inhibitors of the Betaine/GABA Transporter BGT1
Kickinger, Stefanie, Lie, M. E. K., Suemasa, A., Al-Khawaja, A., Fujiwara, K., Watanabe, M., Wilhelmsen, K. S., Falk-Petersen, C. B., Frølund, Bente, Shuto, S., Ecker, G. F. & Wellendorph, Petrine, 2021, In: Frontiers in Chemistry. 9, 13 p., 736457.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Unraveling the Molecular Determinants for GABA Transporter Subtype Selectivity
Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Lie, M. E. K., Bavo, Francesco, Loffler, R., Damgaard, M., Frølund, Bente, Ecker, G. F. & Wellendorph, Petrine, 2020, p. 130A-130A.Research output: Contribution to conference › Conference abstract for conference › Research › peer-review
- Published
Structural and molecular aspects of betaine-GABA transporter 1 (BGT1) and its relation to brain function
Kickinger, S., Hellsberg, E., Frølund, Bente, Schousboe, Arne, Ecker, G. F. & Wellendorph, Petrine, 2019, In: Neuropharmacology. 161, 14 p., 107644.Research output: Contribution to journal › Review › Research › peer-review
- Published
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
- Published
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
- Published
Exploring the orthosteric binding site of the γ-aminobutyric acid type A receptor using 4-(piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation
Krall, J., Jensen, C. H., Sørensen, T. E., Nielsen, Birgitte, Jensen, Anders A., Sander, T., Balle, T. & Frølund, Bente, 15 Jul 2013, In: Journal of Medicinal Chemistry. 56, 16, p. 6536−6540 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs
Krall, J., Jensen, C. H., Bavo, F., Falk-Petersen, C. B., Haugaard, A. S., Vogensen, S. B., Tian, Y., Nittegaard-Nielsen, M., Sigurdardóttir, S. B., Kehler, J., Kongstad, Kenneth Thermann, Gloriam, David E., Clausen, Rasmus Prætorius, Harpsøe, Kasper, Wellendorph, Petrine & Frølund, Bente, 2017, In: Journal of Medicinal Chemistry. 60, 21, p. 9022-9039 18 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
Discovery of α-Substituted Imidazole-4-acetic Acid Analogues as a Novel Class of ρ1 γ-Aminobutyric Acid Type A Receptor Antagonists with Effect on Retinal Vascular Tone
Krall, J., Brygger, B. M., Sigurðardóttir, S. B., Ng, C. K. L., Bundgaard, C., Kehler, J., Nielsen, Birgitte, Bek, T., Jensen, Anders A. & Frølund, Bente, 13 Sep 2016, In: ChemMedChem. 11, 20, p. 2299-2310 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Discovery of 2-(Imidazo[1,2-b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites
Krall, J., Bavo, Francesco, Falk-Petersen, C. B., Jensen, C. H., Nielsen, J. O., Tian, Yongsong, Anglani, V., Kongstad, Kenneth Thermann, Petersen, Louise Piilgaard, Nielsen, Birgitte, Gloriam, David E., Kehler, J., Jensen, Anders A., Harpsøe, Kasper, Wellendorph, Petrine & Frølund, Bente, 14 Mar 2019, In: Journal of Medicinal Chemistry. 62, 5, p. 2798-2813Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
GABAA receptor partial agonists and antagonists: structure, binding mode, and pharmacology
Krall, J., Balle, T., Krogsgaard-Larsen, N., Sørensen, T. E., Krogsgaard-Larsen, Povl, Kristiansen, Uffe & Frølund, Bente, 2015, Diversity and functions of GABA receptors: A tribute to Hanns Möhler, Part A. Vol. 72. p. 201-27 27 p. (Advances in Pharmacology).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
- Published
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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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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