Bente Frølund
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
- 2023
- 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. US202263318852PResearch output: Patent
- Published
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
- Published
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
- Published
Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine
Bavo, Francesco, Kickinger, Stefanie, Lie, M. E. K., Avgerinos, Christos, Wilhelmsen, Kristine Sloth, Wellendorph, Petrine & Frølund, Bente, 2023, In: Medicinal Chemistry Research. 32, p. 2299–2324Research output: Contribution to journal › Journal article › Research › peer-review
- 2022
- Published
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
- Published
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
- Published
The CaMKIIα hub ligand Ph-HTBA promotes neuroprotection after focal ischemic stroke by a distinct molecular interaction
Griem-Krey, Nane, Gauger, Stine Juul, Gowing, E. K., Thiesen, L., Frølund, Bente, Clarkson, A. N. & Wellendorph, Petrine, 2022, In: Biomedicine and Pharmacotherapy. 156, 10 p., 113895.Research output: Contribution to journal › Journal article › Research › peer-review
- 2021
- Published
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
- Published
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
- 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
Molecular Determinants underlying Delta Selective Compound 2 (DS2) Activity at δ-Containing GABAA Receptors
Falk-Petersen, C. B., Rostrup, F., Löffler, R., Buchleihtner, S., Harpsøe, Kasper, Gloriam, David E., Frølund, Bente & Wellendorph, Petrine, 2021, In: Molecular Pharmacology. 100, 1, p. 46-56Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology
Griem-Krey, Nane, Frølund, Bente, Marek, A. & Wellendorph, Petrine, 2021, In: Journal of Labelled Compounds and Radiopharmaceuticals. 64, 2, 77 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based ?-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect
Bavo, Francesco, De-Jong, H., Petersen, Jonas Odgaard, Falk-Petersen, C. B., Löffler, R., Sparrow, E., Rostrup, F., Eliasen, Jannik Nicklas, Wilhelmsen, K. S., Barslund, K., Bundgaard, C., Nielsen, Birgitte, Kristiansen, Uffe, Wellendorph, Petrine, Bogdanov, Y. & Frølund, Bente, 2021, In: Journal of Medicinal Chemistry. 64, 24, p. 17795-17812Research output: Contribution to journal › Journal article › Research › peer-review
- 2020
- 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 journal › Journal article › Research › peer-review
- Published
A CLASS OF SMALL-MOLECULE COMPOUNDS AND THEIR PRODRUGS FOR INTERVENTION WITH CAMK2A, AND THEIR USE IN ACUTE BRAIN INJURIES AND CENTRAL HYPERSOMNIAS
Frølund, Bente, Wellendorph, Petrine & Kornum, Birgitte Rahbek, 2020, Patent No. WO2020151795, 30 Jul 2020, Priority date 21 Jan 2019, Priority No. DK2019PA70040 20190121Research output: Patent
- Published
Compounds for the treatment of acute brain injury
Klein, A. B., Leurs, U., Houlton, J., Clausen, Rasmus Prætorius, Frølund, Bente, Clarkson, A. & Wellendorph, Petrine, 2020, Patent No. CN111989094, 24 Nov 2020, Priority date 1 Feb 2019, Priority No. PCT/DK2019/050041Research output: Patent
- Published
Exploring the molecular determinants for subtype-selectivity of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogs as betaine/GABA transporter 1 (BGT1) substrate-inhibitors
Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Lie, M. E. K., Bavo, Francesco, Loeffler, R., Damgaard, M., Ecker, G. F., Frølund, Bente & Wellendorph, Petrine, 2020, In: Scientific Reports. 10, 1, 15 p., 12992.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Sex-specific alterations in GABA receptor-mediated responses in laterodorsal tegmentum (LDT) are associated with prenatal exposure to nicotine
Eliasen, Jannik Nicklas, Krall, J., Frølund, Bente & Kohlmeier, Kristi Anne, 2020, In: Developmental Neurobiology. 80, 5-6, p. 178-199Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 3975-3990Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- 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
- 2019
- 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. 5797-5809Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
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
- 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
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
- Published
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
- 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
- 2018
- 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 journal › Journal article › Research › peer-review
- Published
Synthesis, pharmacological activity and molecular modeling studies of a series of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogues as betaine/GABA transporter 1 (BGT1) substrate-inhibitors
Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Loeffler, R., Damgaard, M., Eckert, G., Frølund, Bente & Wellendorph, Petrine, 19 Aug 2018.Research output: Contribution to conference › Conference abstract for conference › Research › peer-review
- Published
Pharmacological Characterization of [3H]ATPCA as a Substrate for Studying the Functional Role of the Betaine/GABA Transporter 1 and the Creatine Transporter
Al-Khawaja, A., Haugaard, A. S., Marek, A., Löffler, R., Thiesen, L., Santiveri, M., Damgaard, M., Bundgaard, C., Frølund, Bente & Wellendorph, Petrine, 21 Mar 2018, In: A C S Chemical Neuroscience. 9, 3, p. 545–554Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- 2017
- 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 journal › Journal article › Research › peer-review
- Published
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
- 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 journal › Journal article › Research › peer-review
- Published
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
- 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
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
- 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 proceeding › Book chapter › Research › peer-review
- 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 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
- 2016
- 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
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
- 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
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
- 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 journal › Journal article › Research › peer-review
- 2015
- Published
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
- Published
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
- Published
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
- 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 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
Identification of the first highly selective inhibitor of human GABA transporter GAT3
Damgaard, M., Al-Khawaja, A., Vogensen, S. B., Jurik, A., Sijm, M., Lie, M., Bæk, M. I., Rosenthal, E., Jensen, Anders A., Ecker, G. F., Frølund, Bente, Wellendorph, Petrine & Clausen, Rasmus Prætorius, 2015, In: A C S Chemical Neuroscience. 6, p. 1591-1599 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- 2014
- 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 journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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 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
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
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
- 2013
- Published
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
- 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
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
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
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
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
- Published
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
- Published
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
- 2012
- 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
α4βδ GABA receptors are high-affinity targets for γ-hydroxybutyric acid (GHB)
Absalom, N., Karim, N., Eghorn, L. F., Villumsen, I. S., Bay, T., Bräuner, Hans, Frølund, Bente, Clausen, Rasmus Prætorius, Olsen, Jesper Velgaard, Knudsen, Gitte Moos, Chebib, M. & Wellendorph, Petrine, 14 Aug 2012, In: Proceedings of the National Academy of Sciences USA (PNAS). 109, 33, p. 13404-13409 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2011
- Published
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
- Published
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
- 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
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
- Published
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
- 2010
- Published
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
- 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. 239-262Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
- Published
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
- Published
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
- 2009
- Published
Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC)
Hansen, C. P., Jensen, Anders A., Balle, T., Bitsch-Jensen, K., Hassan, M. M., Liljefors, T. & Frølund, Bente, 2009, In: Bioorganic & Medicinal Chemistry Letters. 19, 1, p. 87-91Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Characterization of GABAA receptor ligands in the rat corticalwedge preparation: evidence for action at extrasynaptic receptors?
Ebert, B., Storustovu, S. I., Mortensen, M. S. & Frølund, Bente, 2009, In: British Journal of Pharmacology. 137, 1, p. 1–8Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- 2008
- Published
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
- 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. 139-147Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research
- 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
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
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
- 2007
- Published
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships
Frølund, Bente, Jensen, L. S., Storustovu, S. I., Stensbøl, T. B., Ebert, B., Kehler, J., Krogsgaard-Larsen, Povl & Liljefors, T., 2007, In: Journal of Medicinal Chemistry. 50, 8, p. 1988-1992Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
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
- 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. 4543-4551Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
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
- 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 conference › Conference abstract for conference › Research › peer-review
- 2006
- 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 proceeding › Book chapter › 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
A novel selective γ-aminobutyric acid transport inhibitor demonstrates a functional role for GABA transporter subtype GAT2/BGT-1 in the CNS
Frølund, Bente, Clausen, Rasmus Prætorius, Larsson, O. M., Schousboe, Arne, Krogsgaard-Larsen, Povl & White, H. S., 2006, In: Neurochemistry International. 48, p. 637–642Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Effekt og bivirkninger: GABA fra A til C.
Frølund, Bente, Madsen, C., Jensen, Anders A., Kristiansen, Uffe & Liljefors, T., 2006, In: Lægemiddelforskning. p. 32-33Research output: Contribution to journal › Journal article › Communication
- Published
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
- Published
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
- 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
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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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