Bente Frølund

Bente Frølund

Professor


  1. Published

    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 journalJournal articleResearchpeer-review

  2. Published

    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. 545–554

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Published

    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 journalJournal articleResearchpeer-review

  4. Published

    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 journalJournal articleResearchpeer-review

  5. Published

    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 journalJournal articleResearchpeer-review

  6. Published

    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 journalJournal articleResearchpeer-review

  7. Published
  8. Published

    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. 17795-17812

    Research output: Contribution to journalJournal articleResearchpeer-review

  9. Published

    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 journalJournal articleResearchpeer-review

  10. Published

    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 conferenceConference abstract for conferenceResearchpeer-review

  11. Published

    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 journalJournal articleResearchpeer-review

  12. Published

    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. 765-768

    Research output: Contribution to journalJournal articleResearch

  13. Published

    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. 150-150

    Research output: Contribution to journalConference abstract in journalResearch

  14. Published

    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 proceedingBook chapterResearchpeer-review

  15. Published

    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. 895–908

    Research output: Contribution to journalJournal articleResearchpeer-review

  16. Published

    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 proceedingBook chapterResearchpeer-review

  17. Published

    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. 5533–5542

    Research output: Contribution to journalJournal articleResearchpeer-review

  18. Published

    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. 3975-3990

    Research output: Contribution to journalJournal articleResearchpeer-review

  19. Published

    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 journalJournal articleResearchpeer-review

  20. Published

    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 proceedingBook chapterResearchpeer-review

  21. Published

    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 journalJournal articleResearchpeer-review

  22. Published

    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 journalJournal articleResearchpeer-review

  23. Published

    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. 625–631

    Research output: Contribution to journalJournal articleResearchpeer-review

  24. Published

    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. 1–8

    Research output: Contribution to journalJournal articleResearchpeer-review

  25. Published

    Equilibrium binding characteristics of [3H]thiomuscimol

    Ebert, B., Frølund, Bente, Diemer, N. & Krogsgaard-Larsen, Povl, 1999, In: Neurochemistry International. 34, p. 427–434

    Research output: Contribution to journalJournal articleResearchpeer-review

  26. Published

    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 journalJournal articleResearchpeer-review

  27. Published

    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. 178-199

    Research output: Contribution to journalJournal articleResearchpeer-review

  28. Published

    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. 5402–5414

    Research output: Contribution to journalJournal articleResearchpeer-review

  29. Published

    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 journalJournal articleResearchpeer-review

  30. Published

    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. 46-56

    Research output: Contribution to journalJournal articleResearchpeer-review

  31. Published

    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 journalJournal articleResearchpeer-review

  32. Published

    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. 4543-4551

    Research output: Contribution to journalJournal articleResearchpeer-review

  33. Published

    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 Verlag

    Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review

  34. Published

    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. 526–533

    Research output: Contribution to journalJournal articleResearchpeer-review

  35. Published

    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 journalLetterResearchpeer-review

  36. Published

    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 journalJournal articleResearchpeer-review

  37. Published

    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. 2454–2468

    Research output: Contribution to journalJournal articleResearchpeer-review

  38. Published

    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 journalJournal articleResearchpeer-review

  39. Published

    GABA-A Receptor Agonists, Partial Agonists and Antagonists

    Frølund, Bente, Krogsgaard-Larsen, Povl & Ebert, B., 1996, The GABA Receptors. 2nd ed. Humana Press

    Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review

  40. Published

    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. 2

    Research output: Contribution to journalJournal articleResearchpeer-review

  41. Published

    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 journalJournal articleResearchpeer-review

  42. Published

    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 Press

    Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review

  43. Published

    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. 4930–4933

    Research output: Contribution to journalJournal articleResearchpeer-review

  44. Published

    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. 355–384

    Research output: Contribution to journalJournal articleResearchpeer-review

  45. Published

    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. US202263318852P

    Research output: Patent

  46. Published
  47. Published

    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. 637–642

    Research output: Contribution to journalJournal articleResearchpeer-review

  48. Published

    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. 520–527

    Research output: Contribution to journalJournal articleResearchpeer-review

  49. Published

    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. 447–449

    Research output: Contribution to journalJournal articleResearchpeer-review

  50. Published

    GABAA Agonists: Resolution and Pharmacology of (+)- and (-)-Isoguvacine Oxide

    Frølund, Bente, Jeppesen, L., Krogsgaard-Larsen, Povl & Hansen, J. J., 1995, In: Chirality. 7, p. 434–438

    Research output: Contribution to journalJournal articleResearchpeer-review

  51. Published

    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. Munksgaard

    Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review

  52. Published

    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. 3287–3296

    Research output: Contribution to journalJournal articleResearchpeer-review

  53. Published

    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 journalReviewResearchpeer-review

  54. Published

    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 journalJournal articleResearchpeer-review

  55. Published

    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. 561–565

    Research output: Contribution to journalJournal articleResearchpeer-review

  56. Published

    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. 427–439

    Research output: Contribution to journalJournal articleResearchpeer-review

  57. Published

    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 journalJournal articleResearchpeer-review

  58. Published

    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. 877–889

    Research output: Contribution to journalJournal articleResearchpeer-review

  59. Published

    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. 5391-8

    Research output: Contribution to journalJournal articleResearchpeer-review

  60. Published

    Effekt og bivirkninger: GABA fra A til C.

    Frølund, Bente, Madsen, C., Jensen, Anders A., Kristiansen, Uffe & Liljefors, T., 2006, In: Lægemiddelforskning. p. 32-33

    Research output: Contribution to journalJournal articleCommunication

  61. Published

    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. 239-262

    Research output: Chapter in Book/Report/Conference proceedingBook chapterEducation

  62. Published

    GABAA-receptoren: Bedre modeller - bedre lægemidler

    Frølund, Bente, Sander, T., Hansen, H. & Balle, T., 2009, In: Lægemiddelforskning. p. 31-33

    Research output: Contribution to journalJournal articleCommunication

  63. Published

    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. 139-147

    Research output: Chapter in Book/Report/Conference proceedingBook chapterResearch

  64. 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. 1988-1992

    Research output: Contribution to journalJournal articleResearchpeer-review

  65. Published

    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 journalJournal articleResearchpeer-review

  66. Published

    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. 5797-5809

    Research output: Contribution to journalJournal articleResearchpeer-review

  67. 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 journalJournal articleResearchpeer-review

  68. 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 journalJournal articleResearchpeer-review

  69. 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. 7380-7395

    Research output: Contribution to journalJournal articleResearchpeer-review

  70. 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. 87-91

    Research output: Contribution to journalJournal articleResearchpeer-review

  71. 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. 6798–6805

    Research output: Contribution to journalJournal articleResearchpeer-review

  72. 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 journalJournal articleResearchpeer-review

  73. 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 journalJournal articleResearchpeer-review

  74. 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 journalJournal articleResearchpeer-review

  75. 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). 232

    Research output: Contribution to journalConference abstract in journalResearch

  76. 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. 1861–1882

    Research output: Contribution to journalJournal articleResearchpeer-review

  77. 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. 8088-8095

    Research output: Contribution to journalJournal articleResearchpeer-review

  78. 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. 515–521

    Research output: Contribution to journalJournal articleResearchpeer-review

  79. 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 journalJournal articleResearchpeer-review

  80. 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 journalJournal articleResearchpeer-review

  81. 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 journalJournal articleResearchpeer-review

  82. 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 journalJournal articleResearchpeer-review

  83. 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 journalJournal articleResearchpeer-review

  84. 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 journalLetterResearchpeer-review

  85. 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. 725-736

    Research output: Contribution to journalJournal articleResearchpeer-review

  86. 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 journalJournal articleResearchpeer-review

  87. 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 conferenceConference abstract for conferenceResearchpeer-review

  88. 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 conferenceConference abstract for conferenceResearchpeer-review

  89. 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 journalJournal articleResearchpeer-review

  90. 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 journalReviewResearchpeer-review

  91. 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 journalJournal articleResearchpeer-review

  92. 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/DK2019/050041

    Research output: Patent

  93. 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 journalJournal articleResearchpeer-review

  94. 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 journalJournal articleResearchpeer-review

  95. 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 conferencePosterResearch

  96. 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 journalJournal articleResearchpeer-review

  97. 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. 2798-2813

    Research output: Contribution to journalJournal articleResearchpeer-review

  98. 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 journalJournal articleResearchpeer-review

  99. 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 proceedingBook chapterResearchpeer-review

  100. 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 journalJournal articleResearchpeer-review

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