Bente Frølund
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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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
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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
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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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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
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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
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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
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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
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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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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
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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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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
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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
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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
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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
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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
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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
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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
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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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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
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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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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
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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
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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
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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
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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
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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
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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
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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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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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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
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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
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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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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
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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
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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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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
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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
ID: 1302625
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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
Research output: Contribution to journal › Journal article › Research › peer-review
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