Povl Krogsgaard-Larsen
Professor, emeritus
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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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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Synaptic and extrasynaptic GABA transporters as targets for anti-epileptic drugs
Madsen, K. K., Clausen, Rasmus Prætorius, Larsson, O. M., Krogsgaard-Larsen, Povl, Schousboe, Arne & White, H. S., 2009, In: Journal of Neurochemistry. 109, Suppl. 1, p. 139-44Research output: Contribution to journal › Journal article › Research › peer-review
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Selective GABA transporter inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABA(A) receptor agonist gaboxadol
Madsen, K. K., Ebert, B., Clausen, Rasmus Prætorius, Krogsgaard-Larsen, Povl, Schousboe, Arne & White, H. S., 1 Jul 2011, In: Journal of Pharmacology and Experimental Therapeutics. 338, 1, p. 214-219Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and pharmacology of 3-isoxazolol amino acids as selective antagonists at group I metabotropic glutamic acid receptors
Madsen, Ulf, Bräuner, Hans, Frydenvang, Karla Andrea, Hvene, L., Johansen, Tommy Nørskov, Nielsen, Birgitte, Sánchez, C., Stensbøl, T. B., Bischoff, F. & Krogsgaard-Larsen, Povl, 2001, In: Journal of Medicinal Chemistry. 44, 7, p. 1051-9 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid
Madsen, Ulf, Frydenvang, Karla Andrea, Ebert, B., Johansen, Tommy Nørskov, Brehm, L. & Krogsgaard-Larsen, Povl, 1996, In: Journal of Medicinal Chemistry. 39, 1, p. 183-90 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Ionotropic excitatory amino acid receptor ligands. Synthesis and pharmacology of a new amino acid AMPA antagonist
Madsen, Ulf, Sløk, F. A., Stensbøl, T. B., Bräuner, Hans, Lützhøft, H. H., Poulsen, M. V., Eriksen, L. & Krogsgaard-Larsen, Povl, Jan 2000, In: European Journal of Medicinal Chemistry. 35, 1, p. 69-76Research output: Contribution to journal › Journal article › Research › peer-review
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Relationship between structure, conformational flexibility, and biological activity of agonists and antagonists at the N-methyl-D-aspartic acid subtype of excitatory amino acid receptors
Madsen, Ulf, Brehm, L., Schaumburg, K., Jørgensen, Flemming Steen & Krogsgaard-Larsen, Povl, 1990, In: Journal of Medicinal Chemistry. 33, 1, p. 374-80 7 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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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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Modification of the philanthotoxin-343 polyamine moiety results in different structure-activity profiles at muscle nicotinic ACh, NMDA and AMPA receptors
Mellor, I. R., Brier, T. J., Pluteanu, F., Strømgaard, Kristian, Saghyan, A., Eldursi, N., Brierley, M. J., Andersen, K., Jaroszewski, J. W., Krogsgaard-Larsen, Povl & Usherwood, P. N. R., Jan 2003, In: Neuropharmacology. 44, 1, p. 70-80 11 p.Research 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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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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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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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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Enzymatic resolution of AMPA by use of alpha-chymotrypsin
Nielsen, Birgitte, Fisker, H., Ebert, B., Madsen, Ulf, Curtis, D. R., Krogsgaard-Larsen, Povl & Hansen, J. J., 1993, In: Bioorganic & Medicinal Chemistry Letters. 3, 1, p. 107–114 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and muscarinic receptor pharmacology of a series of 4,5,6,7-tetrahydroisothiazolo[4,5-c]pyridine bioisosteres of arecoline
Pedersen, H., Bräuner, Hans, Ball, R. G., Frydenvang, Karla Andrea, Meier, E., Bøgesø, K. P. & Krogsgaard-Larsen, Povl, 1999, In: Bioorganic & Medicinal Chemistry. 7, 5, p. 795-809 15 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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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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Aryl and cycloalkyl analogues of AMPA: synthetic, pharmacological and stereochemical aspects
Skjærbæk, N., Brehm, L., Johansen, Tommy Nørskov, Hansen, L. M., Nielsen, Birgitte, Ebert, B., Søby, K., Stensbøl, T. B., Falch, E. & Krogsgaard-Larsen, Povl, 1998, In: Bioorganic & Medicinal Chemistry. 6, 1, p. 119-131 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structural and stereochemical requirements for activation and blocade of excitatory amino acid receptors
Sløk, F. A., Bräuner, Hans, Stensbøl, T. B., Johansen, Tommy Nørskov, Ebert, B., Mortensen, M., Nielsen, Birgitte, Madsen, Ulf, Brehm, L., Falch, E. & Krogsgaard-Larsen, Povl, 2001, Medicinal Chemistry into the Millenium. Campbell, M. M. & Blagbrough, I. S. (eds.). UK: Royal Society of Chemistry, p. 52-64 13 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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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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Stereochemistry and molecular pharmacology of (S)-thio-ATPA, a new potent and selective GluR5 agonist
Stensbøl, T. B., Jensen, H. S., Nielsen, Birgitte, Johansen, Tommy Nørskov, Egebjerg, J., Frydenvang, Karla Andrea & Krogsgaard-Larsen, Povl, 2001, In: European Journal of Pharmacology. 411, 3, p. 245-53 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Novel 1-hydroxyazole bioisosteres of glutamic acid. Synthesis, protolytic properties, and pharmacology
Stensbøl, T. B., Uhlmann, P., Morel, S., Eriksen, B. L., Felding, J., Kromann, H., Hermit, M. B., Greenwood, J. R., Braüner-Osborne, H., Madsen, Ulf, Junager, F., Krogsgaard-Larsen, Povl, Begtrup, M., Vedsø, P. & Bräuner, Hans, 3 Jan 2002, In: Journal of Medicinal Chemistry. 45, 1, p. 19-31Research output: Contribution to journal › Journal article › Research › peer-review
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Analogues of neuroactive polyamine wasp toxins that lack inner basic sites exhibit enhanced antagonism toward a muscle-type mammalian nicotinic acetylcholine receptor
Strømgaard, Kristian, Brierley, M. J., Andersen, K., Sløk, F. A., Mellor, I. R., Usherwood, P. N., Krogsgaard-Larsen, Povl & Jaroszewski, J. W., 16 Dec 1999, In: Journal of Medicinal Chemistry. 42, 25, p. 5224-5234 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Recent advances in the medicinal chemistry of polyamine toxins
Strømgaard, Kristian, Andersen, K., Krogsgaard-Larsen, Povl & Jaroszewski, J. W., Nov 2001, In: Mini - Reviews in Medicinal Chemistry. 1, 4, p. 317-338 22 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Solid-phase synthesis and biological evaluation of a combinatorial library of philanthotoxin analogues
Strømgaard, Kristian, Brier, T. J., Andersen, K., Mellor, I. R., Saghyan, A., Tikhonov, D., Usherwood, P. N., Krogsgaard-Larsen, Povl & Jaroszewski, J. W., 16 Nov 2000, In: Journal of Medicinal Chemistry. 43, 23, p. 4526-4533 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Solid phase synthesis and biological evaluation of enantiomerically pure wasp toxin analogues PhTX-343 and PhTX-12
Strømgaard, Kristian, Bjørnsdottir, I., Andersen, K., Brierley, M. J., Rizoli, S., Eldursi, N., Mellor, I. R., Usherwood, P. N., Hansen, S. H., Krogsgaard-Larsen, Povl & Jaroszewski, J. W., Feb 2000, In: Chirality. 12, 2, p. 93-102 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A versatile method for solid phase synthesis of polyamines: neuroactive polyamine toxins as example
Strømgaard, Kristian, Andersen, K., Ruhland, T., Krogsgaard-Larsen, Povl & Jaroszewski, J. W., 2001, In: Synthesis. 6, p. 877-884 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Solid-phase synthesis and pharmacological evaluation of analogues of PhTX-12-A potent and selective nicotinic acetylcholine receptor antagonist
Strømgaard, Kristian, Mellor, I. R., Andersen, K., Neagoe, I., Pluteanu, F., Usherwood, P. N. R., Krogsgaard-Larsen, Povl & Jaroszewski, J. W., 22 Apr 2002, In: Bioorganic & Medicinal Chemistry Letters. 12, 8, p. 1159-1162 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and in vitro pharmacology at AMPA and kainate preferring glutamate receptors of 4-heteroarylmethylidene glutamate analogues
Valgeirsson, J., Christensen, J. K., Kristensen, Anders Skov, Pickering, Darryl S, Nielsen, Birgitte, Fischer, C., Bräuner, Hans, Nielsen, E. Ø., Krogsgaard-Larsen, Povl & Madsen, U., 2003, In: Bioorganic & Medicinal Chemistry. 11, 20, p. 4341-9 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Resolution, configurational assignment, and enantiopharmacology of 2-amino-3-[3-hydroxy-5-(2-methyl-2H- tetrazol-5-yl)isoxazol-4-yl]propionic acid, a potent GluR3- and GluR4-preferring AMPA receptor agonist
Vogensen, S. B., Jensen, H. S., Stensbøl, T. B., Frydenvang, Karla Andrea, Bang-Andersen, B., Johansen, Tommy Nørskov, Egebjerg, J. & Krogsgaard-Larsen, Povl, 2000, In: Chirality. 12, 10, p. 705-13 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A stereochemical anomaly: the cyclised (R)-AMPA analogue (R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid [(R)-5-HPCA] resembles (S)-AMPA at glutamate receptors
Vogensen, S., Greenwood, J., Varming, A. R., Brehm, L., Pickering, Darryl S, Nielsen, Birgitte, Liljefors, T., Clausen, Rasmus Prætorius, Johansen, Tommy Nørskov & Krogsgaard-Larsen, Povl, 2004, In: Organic & Biomolecular Chemistry. 2, 2, p. 206-213Research output: Contribution to journal › Journal article › Research › peer-review
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Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues
Vogensen, S., Clausen, Rasmus Prætorius, Greenwood, J., Johansen, Tommy Nørskov, Pickering, Darryl S, Nielsen, Birgitte, Ebert, B. & Krogsgaard-Larsen, Povl, 5 May 2005, In: Journal of Medicinal Chemistry. 48, 9, p. 3438-3442Research output: Contribution to journal › Journal article › Research › peer-review
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Selective mGAT2 (BGT-1) GABA Uptake Inhibitor: Design, synthesis and pharmacological characterization
Vogensen, S. B., Jørgensen, L., Madsen, K. K., Borkar, N. N., Wellendorph, Petrine, Skovgaard-Petersen, J., Schousboe, Arne, White, H. S., Krogsgaard-Larsen, Povl & Clausen, Rasmus Prætorius, 11 Feb 2013, In: Journal of Medicinal Chemistry. 56, 5, p. 2160-2164 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A tetrazolyl-substituted subtype-selective AMPA receptor agonist
Vogensen, S. B., Frydenvang, Karla Andrea, Greenwood, J. R., Postorino, G., Nielsen, Birgitte, Pickering, Darryl S, Ebert, B., Bølcho, U., Egebjerg, J., Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Johansen, Tommy Nørskov, Clausen, Rasmus Prætorius & Krogsgaard-Larsen, Povl, 2007, In: Journal of Medicinal Chemistry. 50, 10, p. 2408-2414Research output: Contribution to journal › Journal article › Research › peer-review
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Stereoselective effects of AMOA on non-NMDA receptors expressed in Xenopus oocytes
Wahl, P., Nielsen, Birgitte, Krogsgaard-Larsen, Povl, Hansen, J. J., Schousboe, Arne & Miledi, R., Nov 1992, In: Journal of Neuroscience Research. 33, 3, p. 392-7 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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gamma-Aminobutyric Acid and Glycine Neurotransmitter Transporters
Wellendorph, Petrine, Jacobsen, Julie, Skovgaard-Petersen, J., Jurik, A., Vogensen, S. B., Ecker, G., Schousboe, Arne, Krogsgaard-Larsen, Povl & Clausen, Rasmus Prætorius, 2017, Transporters As Drug Targets.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › 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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3-pyrazolone analogues of the 3-isoxazolol metabotropic excitatory amino acid receptor agonist homo-AMPA. Synthesis and pharmacological testing
Zimmermann, D., Janin, Y. L., Brehm, L., Bräuner, Hans, Ebert, B., Johansen, Tommy Nørskov, Madsen, Ulf & Krogsgaard-Larsen, Povl, 1 Nov 1999, In: European Journal of Medicinal Chemistry. 34, 11, p. 967-976Research output: Contribution to journal › Journal article › Research › peer-review
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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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