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 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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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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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-substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel ¿-aminobutyric acidC receptor agonists
Madsen, C., Jensen, A. A., Liljefors, T., Kristiansen, Uffe, Nielsen, Birgitte, Hansen, C. P., Larsen, M., Ebert, B., Bang-Andersen, B., Krogsgaard-Larsen, Povl & Frølund, Bente, 2007, In: Journal of Medicinal Chemistry. 50, 17, p. 4147-4161Research output: Contribution to journal › Journal article › Research › peer-review
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Differential interactions of 5-(4-piperidyl)-3-isoxazolol analogues with insect γ-aminobutyric acid receptors leading to functional selectivity
Liu, G., Frølund, Bente, Ozoe, F. & Ozoe, Y., 2015, In: Insect Biochemistry and Molecular Biology. 66, p. 64-71 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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GHB analogs confer neuroprotection through specific interaction with the CaMKIIα hub domain
Leurs, U., Klein, A. B., McSpadden, E. D., Griem-Krey, N., Solbak, S. M. Ø., Houlton, J., Villumsen, I. S., Vogensen, S. B., Hamborg, L., Gauger, S. J., Palmelund, L. B., Larsen, A. S. G., Shehata, M. A., Kelstrup, C. D., Olsen, J. V., Bach, A., Burnie, R. O., Kerr, D. S., Gowing, E. K., Teurlings, S. M. W. & 9 others, , 2021, In: Proceedings of the National Academy of Sciences of the United States of America. 118, 31, 9 p., e2108079118.Research output: Contribution to journal › Journal article › Research › peer-review
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Transport of amino acids and GABA analogues via the human proton-coupled amino acid transporter, hPAT1: Characterization of conditions for affinity and transport experiments in Caco-2 cells.
Larsen, M., Larsen, Birger Brodin, Frølund, Bente & Nielsen, C. U., 2008, In: European Journal of Pharmaceutical Sciences. 35, 1-2, p. 86-95Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and Pharmacological Evaluation of [C-11]4-Methoxy-N-[2-(thiophen-2-yl) imidazo[1,2-a] pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the delta-Subunit-Containing gamma-Aminobutyric Acid Type A Receptors
L'Estrade, E. T., Hansen, H. D., Falk-Petersen, C., Haugaard, A., Griem-Krey, Nane, Jung, S., Lueddens, H., Schirmeister, T., Erlandsson, M., Ohlsson, T., Knudsen, Gitte Moos, Herth, Matthias Manfred, Wellendorph, Petrine & Frølund, Bente, May 2019, In: ACS Omega. 4, 5, p. 8846-8851Research output: Contribution to journal › Journal article › Research › peer-review
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Ligands for the GABAA receptor complex
Krogsgaard-Larsen, Povl, Frølund, Bente, Kristiansen, Uffe & Ebert, B., 1 Jan 2001, Glutamate and GABA Receptors and Transporters: Structure, Function and Pharmacology. CRC Press, p. 236-274 39 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Novel (Gamma-Aminobutyric Acid)A Agonists and Partial Agonists
Krogsgaard-Larsen, Povl, Frølund, Bente, Kristiansen, Uffe, Lambert, J. D. C., Falch, E. & Curtis, D. R., 1991, Transmitter Amino Acid Receptors. Barnard, E. A. & Costa, E. (eds.). Raven Press, p. 237–249Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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GABAA agonists and partial agonists
Krogsgaard-Larsen, Povl, Frølund, Bente & Liljefors, T., 2002, In: The Chemical Record. 2, p. 419–430Research output: Contribution to journal › Journal article › Research › peer-review
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GABA(A) and GABA(B) receptor agonists, partial agonists, antagonists and modulators: Design and therapeutic prospects
Krogsgaard-Larsen, Povl, Frølund, Bente, Kristiansen, Uffe, Frydenvang, Karla Andrea & Ebert, B., Nov 1997, In: European Journal of Pharmaceutical Sciences. 5, 6, p. 355-384 30 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Specific GABAA agonists and partial agonists
Krogsgaard-Larsen, Povl, Frølund, Bente & Liljefors, T., 1 Nov 2002, In: Chemical Record. 2, 6, p. 419-430 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
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GABAA Agonists and Partial Agonists: THIP (Gaboxadol) as a Non-Opioid Analgesic and a Novel Type of Hypnotic
Krogsgaard-Larsen, Povl, Frølund, Bente, Liljefors, T. & Ebert, B., 2006, GABA. Enna, S. (ed.). p. 53–71 (Advances in Pharmacology).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Ligands for the GABAA receptor complex
Krogsgaard-Larsen, Povl, Frølund, Bente, Kristiansen, Uffe & Ebert, B., 2002, Glutamate and GABA receptors of AMPA/kainate receptors and transporters. Taylor & Francis, p. 236–274Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research
- Published
GABA A agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic
Krogsgaard-Larsen, Povl, Frølund, Bente, Liljefors, T. & Ebert, B., 15 Oct 2004, In: Biochemical Pharmacology. 68, 8, p. 1573-1580 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Inhibitors of γ-aminobutyric acid transport as experimental tools and therapeutic agents
Krogsgaard-Larsen, Povl, Frølund, Bente & Falch, E., 1998, Methods in enzymology. p. 165–175 (Methods in Enzymology).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research
- Published
GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects
Krogsgaard-Larsen, Povl, Frølund, Bente, Jørgensen, Flemming Steen & Schousboe, Arne, 1994, In: Journal of Medicinal Chemistry. 37, 16, p. 2489-505 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects
Krogsgaard-Larsen, Povl, Frølund, Bente & Frydenvang, Karla Andrea, 2000, In: Current Pharmaceutical Design. 6, 12, p. 1193-209 17 p.Research output: Contribution to journal › Journal article › 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
- Published
Potent 4-Arylalkyl-Substituted 3-Isothiazolol GABAA Competitive/Noncompetitive Antagonists: Synthesis and Pharmacology
Krehan, D., i Storustovu, S., Liljefors, T., Ebert, B., Nielsen, Birgitte, Krogsgaard-Larsen, Povl & Frølund, Bente, 2006, In: Journal of Medicinal Chemistry. 49, p. 1388–1396Research output: Contribution to journal › Journal article › 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., 2003, In: Bioorganic and Medicinal Chemistry. 11, p. 4891–4896Research output: Contribution to journal › Journal article › Research › peer-review
- 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
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
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
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
- 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
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
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
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
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
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
- 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
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
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
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
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
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
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
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
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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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