Ulf Madsen
Associate Professor emeritus
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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(S)-homo-AMPA, a specific agonist at the mGlu6 subtype of metabotropic glutamic acid receptors
Ahmadian, H., Nielsen, Birgitte, Bräuner, Hans, Johansen, Tommy Nørskov, Stensbøl, T. B., Sløk, F. A., Sekiyama, N., Nakanishi, S., Krogsgaard-Larsen, Povl & Madsen, Ulf, 24 Oct 1997, In: Journal of Medicinal Chemistry. 40, 22, p. 3700-5Research output: Contribution to journal › Journal article › Research › peer-review
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Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO)
Bjerrum, E. J., Kristensen, Anders Skov, Pickering, D. S., Greenwood, J. R., Nielsen, Birgitte, Liljefors, T., Schousboe, Arne, Bräuner, Hans, Madsen, Ulf & Pickering, Darryl S, 2003, In: Journal of Medicinal Chemistry. 46, 11, p. 2246-9 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structural and stereochemical requirements for interactions with subtypes of central excitatory amino acid receptors
Brehm, L., Christensen, I. T., Nielsen, Birgitte, Reinhardt, A., Ebert, B., Madsen, Ulf, Jørgensen, Flemming Steen, Hansen, J. J. & Krogsgaard-Larsen, Povl, 1990, Frontiers in Drug Research; Alfred Benzon Symposium 28. Jensen, B., Jørgensen, F. S. & Kofod, H. (eds.). Copenhagen: Munksgaard , p. 92-105 14 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Ligands for glutamate receptors: design and therapeutic prospects
Bräuner, Hans, Egebjerg, J., Nielsen, E. O., Madsen, Ulf & Krogsgaard-Larsen, Povl, 13 Jul 2000, In: Journal of Medicinal Chemistry. 43, 14, p. 2609-45Research output: Contribution to journal › Journal article › Research › peer-review
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New analogues of ACPD with selective activity for group II metabotropic glutamate receptors
Bräuner, Hans, Madsen, Ulf, Mikiciuk-Olasik, E. & Curry, K., 13 Aug 1997, In: European Journal of Pharmacology. 332, 3, p. 327-31 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Unprecedented migration of N-alkoxycarbonyl groups in protected pyroglutaminol
Bunch, Lennart, Norrby, P., Frydenvang, Karla Andrea, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2001, In: Organic Letters. 3, 3, p. 433-5 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and receptor binding affinity of new selective GluR5 ligands
Bunch, Lennart, Johansen, T. H., Bräuner, Hans, Stensbøl, T. B., Johansen, Tommy Nørskov, Krogsgaard-Larsen, Povl & Madsen, Ulf, Apr 2001, In: Bioorganic & Medicinal Chemistry. 9, 4, p. 875-9Research output: Contribution to journal › Journal article › Research › peer-review
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Rational design, synthesis, and pharmacological evaluation of 2-azanorbornane-3-exo,5-endo-dicarboxylic acid: a novel conformationally restricted glutamic acid analogue
Bunch, Lennart, Liljefors, T., Greenwood, J. R., Frydenvang, Karla Andrea, Bräuner, Hans, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2003, In: Journal of Organic Chemistry. 68, 4, p. 1489-95 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Mixed cyano-gilman cuprates - Advances in conjugate addition to alpha,beta-unsaturated pyroglutaminol
Bunch, Lennart, Krogsgaard-Larsen, Povl & Madsen, Ulf, Jan 2002, In: Synthesis. 1, p. 31-33Research output: Contribution to journal › Journal article › Research › peer-review
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Regioselective lithiation and functionalization of 3-(benzyloxy)isothiazole: Application to the synthesis of thioibotenic acid
Bunch, Lennart, Krogsgaard-Larsen, Povl & Madsen, Ulf, 5 Apr 2002, In: Journal of Organic Chemistry. 67, 7, p. 2375-2377Research output: Contribution to journal › Journal article › Research › peer-review
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Excitatory amino acid agonists and partial agonists
Christensen, I. T., Reinhardt, A., Nielsen, B., Ebert, B., Madsen, Ulf, Nielsen, E. O., Brehm, L. & Krogsgaard-Larsen, Povl, 1989, In: Drug Design and Delivery. 5, 1, p. 57-71 15 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to homoibotenic acid
Christensen, I. T., Ebert, B., Madsen, Ulf, Nielsen, Birgitte, Brehm, L. & Krogsgaard-Larsen, Povl, 18 Sep 1992, In: Journal of Medicinal Chemistry. 35, 19, p. 3512-3519 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Excitatory Amino acid agonists and parital agonists
Christensen, I. T., Reinhardt, A., Nielsen, Birgitte, Ebert, B., Madsen, Ulf, Nielsen, E. Ø., Brehm, L. & Krogsgaard-Larsen, Povl, 1989, In: drug design and delivery. 5, p. 57-71 15 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and pharmacology of 3-hydroxy-delta2-isoxazoline-cyclopentane analogues of glutamic acid
Conti, P., De Amici, M., Bräuner, Hans, Madsen, Ulf, Toma, L. & De Micheli, C., Nov 2002, In: Farmaco. 57, 11, p. 889-95Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and pharmacology of a new AMPA-kainate receptor agonist with potent convulsant activity
Conti, P., De Amici, M., De Sarro, G., Stensbøl, T. B., Bräuner, Hans, Madsen, Ulf & De Micheli, C., 24 Sep 1998, In: Journal of Medicinal Chemistry. 41, 20, p. 3759-62Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists
Conti, P., De Amici, M., De Sarro, G., Rizzo, M., Stensbøl, T. B., Bräuner, Hans, Madsen, Ulf, Toma, L. & De Micheli, C., 7 Oct 1999, In: Journal of Medicinal Chemistry. 42, 20, p. 4099-107Research output: Contribution to journal › Journal article › Research › peer-review
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Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization
Conti, P., Pinto, A., Tamborini, L., Madsen, Ulf, Nielsen, Birgitte, Bräuner, Hans, Hansen, K. B., Landucci, E., Pellegrini-Giampietro, D. E., De Sarro, G., Donato Di Paola, E. & De Micheli, C., 2010, In: ChemMedChem. 5, 9, p. 1465-1475Research output: Contribution to journal › Journal article › Research › peer-review
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Design of novel conformationally restricted analogues of glutamic acid
Conti, P., De Amici, M., Roda, G., Vistoli, G., Stensbøl, T. B., Bräuner, Hans, Madsen, Ulf, Toma, L. & De Micheli, C., 24 Feb 2003, In: Tetrahedron. 59, 9, p. 1443-1452 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of novel N1-substituted bicyclic pyrazole amino acids and evaluation of their interaction with glutamate receptors
Conti, P., Grazioso, G., di Ventimiglia, S. J., Pinto, A., Roda, G., Madsen, Ulf, Bräuner, Hans, Nielsen, Birgitte, Costagli, C. & Galli, A., Jun 2005, In: Chemistry & Biodiversity. 2, 6, p. 748-57Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis, binding affinity at glutamic acid receptors, neuroprotective effects, and molecular modeling investigation of novel dihydroisoxazole amino acids
Conti, P., De Amici, M., Grazioso, G., Roda, G., Pinto, A., Hansen, K. B., Nielsen, Birgitte, Madsen, Ulf, Bräuner, Hans, Egebjerg, J., Vestri, V., Pellegrini-Giampietro, D. E., Sibille, P., Acher, F. C. & De Micheli, C., 6 Oct 2005, In: Journal of Medicinal Chemistry. 48, 20, p. 6315-25Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids
Conti, P., De Amici, M., Joppolo Di Ventimiglia, S., Stensbøl, T. B., Madsen, Ulf, Bräuner, Hans, Russo, E., De Sarro, G., Bruno, G. & De Micheli, C., 3 Jul 2003, In: Journal of Medicinal Chemistry. 46, 14, p. 3102-8Research output: Contribution to journal › Journal article › Research › peer-review
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Design, synthesis, and pharmacological characterization of novel, potent NMDA receptor antagonists
Conti, P., De Amici, M., Grazioso, G., Roda, G., Barberis Negra, F. F., Nielsen, Birgitte, Stensbøl, T. B., Madsen, Ulf, Bräuner, Hans, Frydenvang, Karla Andrea, De Sarro, G., Toma, L. & De Micheli, C., 30 Dec 2004, In: Journal of Medicinal Chemistry. 47, 27, p. 6740-8 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Design of Cyclopentaisoxazoline Amino Acids as Conformationally Constrained Agonists at Glutamate Receptors
Conti, P., De Amici, M., Grazioso, G., Roda, G., Stensbøl, T. B., Bräuner, Hans, Madsen, Ulf, Toma, L. & De Micheli, C., 14 Nov 2003, In: European Journal of Organic Chemistry. 22, p. 4455-4461 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and pharmacological characterization at glutamate receptors of erythro- and threo-tricholomic acid and homologues thereof
Conti, P., De Amici, M., Roda, G., Pinto, A., Tamborini, L., Madsen, Ulf, Nielsen, Birgitte, Bräuner, Hans & De Micheli, C., 2007, In: Tetrahedron. 63, 10, p. 2249-2256Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and pharmacological evaluation of novel conformationally constrained homologues of glutamic acid
Conti, P., Caligiuri, A., Pinto, A., Roda, G., Tamborini, L., Nielsen, Birgitte, Madsen, Ulf, Frydenvang, Karla Andrea, Colombo, A. & De Micheli, C., 2007, In: European Journal of Medicinal Chemistry. 42, 8, p. 1059-1068Research output: Contribution to journal › Journal article › Research › peer-review
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Subtype-selective excitatory amino acid receptor agonists and antagonists derived from ibotenic acid
Ebert, B., Lund, Trine Meldgaard, Madsen, Ulf, Brehm, L. & Krogsgaard-Larsen, Povl, 1992, New leads and targets in drug research: Alfred Benzon Symposium 33. Krogsgaard-Larsen, P., Christensen, S. B. & Kofod, H. (eds.). Copenhagen, p. 340-351 11 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Molecular pharmacology of the AMPA agonist, (S)-2-amino-3-(3-hydroxy-5-phenyl-4-isoxazolyl)propionic acid [(S)-APPA] and the AMPA antagonist, (R)-APPA
Ebert, B., Madsen, Ulf, Lund, Trine Meldgaard, Lenz, S. M. & Krogsgaard-Larsen, Povl, Jun 1994, In: Neurochemistry International. 24, 6, p. 507-15 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular pharmacology of cortical and spinal AMPA receptors
Ebert, B., Madsen, Ulf, Lund, Trine Meldgaard, Holm, T. & Krogsgaard-Larsen, Povl, 1 Jan 1992, In: Molecular Neuropharmacology. 2, 1, p. 47-49 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Tetrazolyl isoxazole amino acids as ionotropic glutamate receptor antagonists: synthesis, modelling and molecular pharmacology
Frølund, Bente, Greenwood, J. R., Holm, M. M., Egebjerg, J., Madsen, Ulf, Nielsen, Birgitte, Bräuner, Hans, Stensbøl, T. B. & Krogsgaard-Larsen, Povl, 15 Sep 2005, In: Bioorganic & Medicinal Chemistry. 13, 18, p. 5391-8Research output: Contribution to journal › Journal article › Research › peer-review
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GABA and glutamic acid receptor ligands
Frølund, Bente & Madsen, Ulf, 2010, Textbook of drug design and discovery. Krogsgaard-Larsen, P., Strømgaard, K. & Madsen, U. (eds.). 4 ed. Boca Raton: CRC Press, p. 239-262Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
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Glutamate receptor ligands: synthesis, stereochemistry, and enantiopharmacology of methylated 2-aminoadipic acid analogs
Guldbrandt, M., Johansen, Tommy Nørskov, Frydenvang, Karla Andrea, Bräuner, Hans, Stensbøl, T. B., Nielsen, Birgitte, Karla, R., Santi, F., Krogsgaard-Larsen, Povl & Madsen, Ulf, 2002, In: Chirality. 14, 4, p. 351-63 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Partial agonism and antagonism of the ionotropic glutamate receptor iGLuR5: Structures of the ligand-bining core in complex with domoic acid and 2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]propionic acid
Hald, H., Naur, P., Pickering, Darryl S, Sprogøe, D., Madsen, Ulf, Timmermann, D. B., Ahring, P. K., Liljefors, T., Schousboe, Arne, Egebjerg, J., Gajhede, Michael & Kastrup, Jette Sandholm Jensen, 2007, In: Journal of Biological Chemistry. 282, 35, p. 25726-25736Research output: Contribution to journal › Journal article › Research › peer-review
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Isoxazole amino acids as glutamic acid receptor agonists: conformational and stereochemical aspects
Hansen, J. J., Madsen, Ulf, Nielsen, E. Ø., Nielsen, Birgitte, Brehm, L. & Krogsgaard-Larsen, Povl, 1989, New Methods in Drug Research. Makriayannis, A. (ed.). Barcelona: Prous Scientific Publishers, Vol. 3. p. 73-101 29 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Ibotenic acid and thioibotenic acid: a remarkable difference in activity at group III metabotropic glutamate receptors
Hermit, M. B., Greenwood, J. R., Nielsen, Birgitte, Bunch, Lennart, Jørgensen, Charlotte Grube, Vestergaard, H. T., Stensbøl, T. B., Sanchez, C., Krogsgaard-Larsen, Povl, Madsen, Ulf & Bräuner, Hans, 23 Feb 2004, In: European Journal of Pharmacology. 486, 3, p. 241-50Research output: Contribution to journal › Journal article › Research › peer-review
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Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid
Johansen, Tommy Nørskov, Ebert, B., Bräuner, Hans, Didriksen, M., Christensen, I. T., Søby, K. K., Madsen, Ulf, Krogsgaard-Larsen, Povl & Brehm, L., 12 Mar 1998, In: Journal of Medicinal Chemistry. 41, 6, p. 930-9Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and structure-activity studies on acidic amino acids and related diacids as NMDA receptor ligands
Johansen, Tommy Nørskov, Frydenvang, Karla Andrea, Ebert, B., Krogsgaard-Larsen, Povl & Madsen, Ulf, 1994, In: Journal of Medicinal Chemistry. 37, 20, p. 3252-62 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA
Johansen, Tommy Nørskov, Stensbøl, T. B., Nielsen, Birgitte, Vogensen, S. B., Frydenvang, Karla Andrea, Sløk, F. A., Bräuner, Hans, Madsen, Ulf & Krogsgaard-Larsen, Povl, 2001, In: Chirality. 13, 9, p. 523-32 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Excitatory amino acid receptor antagonists: resolution, absolute stereochemistry, and pharmacology of (S)- and (R)-2-amino-2-(5-tert-butyl-3-hydroxyisoxazol-4-yl)acetic acid (ATAA)
Johansen, Tommy Nørskov, Frydenvang, Karla Andrea, Ebert, B., Madsen, Ulf & Krogsgaard-Larsen, Povl, 1997, In: Chirality. 9, 5-6, p. 529-36 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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2-Amino-3-(3-hydroxy-1,2,5-thiadiazol-4-yl)propionic acid: resolution, absolute stereochemistry and enantiopharmacology at glutamate receptors
Johansen, Tommy Nørskov, Janin, Y. L., Nielsen, Birgitte, Frydenvang, Karla Andrea, Bräuner, Hans, Stensbøl, T. B., Vogensen, S. B., Madsen, Ulf & Krogsgaard-Larsen, Povl, 2002, In: Bioorganic & Medicinal Chemistry. 10, 7, p. 2259-66 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Stereostructure-activity studies on agonists at the AMPA and kainate subtypes of ionotropic glutamate receptors
Johansen, Tommy Nørskov, Greenwood, J. R., Frydenvang, Karla Andrea, Madsen, Ulf & Krogsgaard-Larsen, Povl, 2003, In: Chirality. 15, 2, p. 167-79 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Erratum: Synthesis and pharmacology of glutamate receptor ligands: New isothiazole analogues of ibotenic acid (Organic and Biomolecular Chemistry (2007) 5 DOI:10.1039/b615162k)
Jørgensen, Charlotte Grube, Clausen, Rasmus Prætorius, Hansen, K. B., Bräuner, Hans, Nielsen, Birgitte, Metzler, B., Kehler, J., Krogsgaard-Larsen, Povl & Madsen, Ulf, 2007, In: Organic and Biomolecular Chemistry. 5, 5, p. 848 1 p.Research output: Contribution to journal › Comment/debate › Research › peer-review
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Synthesis and pharmacology of glutamate receptor ligands: new isothiazole analogues of ibotenic acid
Jørgensen, Charlotte Grube, Clausen, Rasmus Prætorius, Hansen, K. B., Bräuner, Hans, Nielsen, Birgitte, Metzler, B., Kehler, J., Krogsgaard-Larsen, Povl & Madsen, Ulf, 2007, In: Organic & Biomolecular Chemistry. 5, 3, p. 463-471Research output: Contribution to journal › Journal article › Research › peer-review
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Novel 5-substituted 1-pyrazolol analogues of ibotenic acid: synthesis and pharmacology at glutamate receptors
Jørgensen, Charlotte Grube, Bräuner, Hans, Nielsen, Birgitte, Kehler, J., Clausen, Rasmus Prætorius, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2007, In: Bioorganic & Medicinal Chemistry. 15, 10, p. 3524-3538Research output: Contribution to journal › Journal article › Research › peer-review
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Analogues of 3-Hydroxyisoxazole-Containing Glutamate Receptor Ligands Based on the 3-Hydroxypyrazole-Moiety: Design, Synthesis and Pharmacological Characterization
Jørgensen, L., Nielsen, Birgitte, Pickering, Darryl S, Kristensen, Anders Skov, Frydenvang, Karla Andrea, Madsen, Ulf & Clausen, Rasmus Prætorius, 2014, In: Neurochemical Research. 39, 10, p. 1895-1905 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity relationships for negative allosteric mGluR5 modulators
Kaae, B. H., Harpsøe, Kasper, Kvist, T., Mathiesen, Jesper M., Mølck, C., Gloriam, David E., Jimenez, H. N., Uberti, M. A., Nielsen, S. M., Nielsen, Birgitte, Bräuner, Hans, Sauerberg, P., Clausen, Rasmus Prætorius & Madsen, Ulf, 2012, In: ChemMedChem. 7, 3, p. 440-451Research output: Contribution to journal › Journal article › Research › peer-review
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Design and characterization of dimeric ligands cross-linking two identical modulatory AMPA receptor sites
Kaae, B. H., Harpsøe, Kasper, Sanz, A. C., Pickering, Darryl S, Sauerberg, P., Clausen, Rasmus Prætorius, Kastrup, Jette Sandholm Jensen, Liljefors, T. & Madsen, Ulf, 19 Aug 2007, In: American Chemical Society. Abstracts of Papers (at the National Meeting). 234Research output: Contribution to journal › Conference abstract in journal › Research
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Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites
Kaae, B. H., Harpsøe, Kasper, Kastrup, Jette Sandholm Jensen, Sanz, A. C., Pickering, Darryl S, Metzler, B., Clausen, Rasmus Prætorius, Gajhede, Michael, Sauerberg, P., Liljefors, T. & Madsen, Ulf, 2007, In: Chemistry & Biology. 14, 11, p. 1294-303 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Design of excitatory amino acid receptor agonists, partial agonists and antagonists: Ibotenic acid as a key lead structure
Krogsgaard-Larsen, Povl, Ebert, B., Lund, Trine Meldgaard, Bräuner, Hans, Sloøk, F. A., Johansen, Tommy Nørskov, Brehm, L. & Madsen, Ulf, 10 Sep 1996, In: European Journal of Medicinal Chemistry. 31, 7-8, p. 515-537 23 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular pharmacology of excitatory amino acid receptors: conformational and stereochemical requirements
Krogsgaard-Larsen, Povl, Madsen, Ulf, Nielsen, Birgitte, Hansen, J. J., Nielsen, E. Ø., Brehm, L. & Curtis, D. R., 1987, Proceedings of the X'th International Congress of Pharmacology. Rand, M. J. & Raper, C. (eds.). Elsevier, p. 113-116 4 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Medicinal chemical and pharmacological focus on GABA and glutamic acid receptors in neurodegenerative disorders
Krogsgaard-Larsen, Povl, Hedegaard, A., Nielsen, L., Nielsen, Birgitte, Madsen, Ulf, Brehm, L., Falch, E., Hjeds, H. & Hansen, J. J., 1989, Trends in Medicinal Chemistry '88. van der Goot, H., Domány, G., Pallos, L. & Timmerman, H. (eds.). Elsevier, Amsterdam, p. 429-452 24 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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