U. Madsen

发表

Lessons from more than 80 structures of the GluA2 ligand-binding domain in complex with agonists, antagonists and allosteric modulators

J. Kastrup, Jacob Pøhlsgaard, K. Frydenvang, 2011, Neuropharmacology.

Structure–Activity Relationships for Negative Allosteric mGluR5 Modulators

Christina Mølck, Hans Bräuner-Osborne, Kasper Harpsøe, 2012, ChemMedChem.

Synthesis and pharmacological characterization at glutamate receptors of erythro-and threo-tricholomic acid and homologues thereof

G. Roda, A. Pinto, L. Tamborini, 2007 .

Analogues of homoibotenic acid show potent and selective activity following sensitisation by quisqualic acid.

U. Madsen, B. Ebert, H. Vestergaard, 2004, European journal of pharmacology.

Synthesis and in vitro pharmacology at AMPA and kainate preferring glutamate receptors of 4-heteroarylmethylidene glutamate analogues.

P. Krogsgaard‐Larsen, A. Kristensen, D. Pickering, 2003, Bioorganic & medicinal chemistry.

Structural Determinants for AMPA Agonist Activity of Aryl or Heteroaryl Substituted AMPA Analogues. Synthesis and Pharmacology

U. Sørensen, P. Krogsgaard‐Larsen, E. Falch, 2001, Archiv der Pharmazie.

Excitatory amino-acid receptor agonists. Synthesis and pharmacology of analogues of 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid

P. Krogsgaard‐Larsen, U. Madsen, B. Ebert, 1997 .

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).

P. Krogsgaard‐Larsen, K. Frydenvang, U. Madsen, 1997, Chirality.

Synthesis and pharmacology of highly selective carboxy and phosphono isoxazole amino acid AMPA receptor antagonists.

P. Krogsgaard‐Larsen, B. Bang-Andersen, U. Madsen, 1996, Journal of medicinal chemistry.

The non-depolarizing D-form of bromohomoibotenic acid enhances depolarizations evoked by the L-form or quisqualate.

P. Krogsgaard‐Larsen, U. Madsen, B. Ebert, 1993, European journal of pharmacology.

Excitatory amino acid receptor atagonists: synthesis and pharmacology of 3-(carboxymethoxy)isoxazoles derived from AMPA

P. Krogsgaard‐Larsen, T. B. Rasmussen, U. Madsen, 1993 .

Enzymatic resolution of AMPA by use of α-chymotrypsin

D. R. Curtis, P. Krogsgaard‐Larsen, U. Madsen, 1993 .

Synthesis and pharmacology of (RS)-2-amino-3-(3-hydroxy-5-trifluoromethyl-4-isoxazolyl)propionic acid, a potent AMPA receptor agonist

E. Wong, P. Krogsgaard‐Larsen, U. Madsen, 1992 .

Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites.

T. Liljefors, J. Kastrup, M. Gajhede, 2007, Chemistry & biology.

Novel 5-substituted 1-pyrazolol analogues of ibotenic acid: synthesis and pharmacology at glutamate receptors.

J. Kehler, P. Krogsgaard‐Larsen, R. Clausen, 2007, Bioorganic & medicinal chemistry.

Ligands for Glutamate Receptors: Design and Therapeutic Prospects

P. Krogsgaard‐Larsen, U. Madsen, J. Egebjerg, 2000 .

Synthesis and pharmacology of glutamate receptor ligands: new isothiazole analogues of ibotenic acid.

J. Kehler, P. Krogsgaard‐Larsen, K. Hansen, 2007, Organic & biomolecular chemistry.

4-Alkylated homoibotenic acid (HIBO) analogues: Versatile pharmacological agents with diverse selectivity profiles towards metabotropic and ionotropic glutamate receptor subtypes

D. Pickering, H. Bräuner‐Osborne, U. Madsen, 2005, Neuropharmacology.

Agonist discrimination between AMPA receptor subtypes

A. Schousboe, T. Banke, D. Pickering, 2000, Neuroreport.

Characterization of a new AMPA receptor radioligand, [3H]2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid.

P. Krogsgaard‐Larsen, N. Diemer, U. Madsen, 1999, European journal of pharmacology.

Differentiation of in vivo effects of AMPA and NMDA receptor ligands using drug discrimination methods and convulsant/anticonvulsant activity.

P. Krogsgaard‐Larsen, C. Sánchez, J. Arnt, 1995, European journal of pharmacology.

Rigid nonproteinogenic cyclic amino acids as ligands for glutamate receptors: trans-tris(homoglutamic) acids.

G. Höfner, H. Bräuner‐Osborne, U. Madsen, 2005, Chirality.

Pharmacological Characterization and Modeling of the Binding Sites of Novel 1,3-Bis(pyridinylethynyl)benzenes as Metabotropic Glutamate Receptor 5-Selective Negative Allosteric Modulators

Christina Mølck, David E. Gloriam, Hans Bräuner-Osborne, 2012, Molecular Pharmacology.

Design, synthesis and in vitro pharmacology of GluK1 and GluK3 antagonists. Studies towards the design of subtype-selective antagonists through 2-carboxyethyl-phenylalanines with substituents interacting with non-conserved residues in the GluK binding sites.

L. Olsen, D. Pickering, J. Kristensen, 2014, Bioorganic & medicinal chemistry.

GABA and Glutamate Receptor Ligands and their Therapeutic Potential in CNS Disorders

T. Liljefors, J. Greenwood, P. Krogsgaard‐Larsen, 2010 .

Stereostructure-activity studies on agonists at the AMPA and kainate subtypes of ionotropic glutamate receptors.

J. Greenwood, P. Krogsgaard‐Larsen, K. Frydenvang, 2003, Chirality.

Ligands for glutamate receptors: design and therapeutic prospects.

P. Krogsgaard‐Larsen, H. Bräuner‐Osborne, U. Madsen, 2000, Journal of medicinal chemistry.

Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.

C. Mathiesen, E. Nielsen, A. Kristensen, 2004, Journal of medicinal chemistry.

A textbook of drug design and development

Tommy Liljefors, T. Liljefors, P. Krogsgaard‐Larsen, 1996 .

Rapid Synthesis of Aryl Azides from Aryl Halides under Mild Conditions.

U. Madsen, Xifu Liang, F. Bjoerkling, 2005 .

Synthesis, binding affinity at glutamic acid receptors, neuroprotective effects, and molecular modeling investigation of novel dihydroisoxazole amino acids.

F. Acher, K. Hansen, G. Roda, 2005, Journal of medicinal chemistry.

Synthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid.

A. Pinto, L. Tamborini, P. Conti, 2008, Journal of medicinal chemistry.

Chemistry of 3-oxygenated isoxazoles. Formation and X-ray analysis of ethyl (RS)-6-tert-butyl-5-methyl-4-oxo-2,3-dihydro-4H-1,3-oxazine-2-carboxylate, an isoxazol-3(2H)-one rearrangement product

P. Krogsgaard‐Larsen, U. Madsen, L. Brehm, 1991 .

Synthesis of new isoxazoline-based acidic amino acids and investigation of their affinity and selectivity profile at ionotropic glutamate receptors.

A. Pinto, L. Tamborini, P. Conti, 2011, European journal of medicinal chemistry.

Unambiguous synthesis of 1-methyl-3-hydroxypyrazoles

P. Krogsgaard‐Larsen, J. Ehrhardt, U. Madsen, 1998 .

Heterocyclic excitatory amino acids. Synthesis and biological activity of novel analogues of AMPA.

E. Wong, U. Madsen, 1992, Journal of medicinal chemistry.

Excitatory amino acids. Improved synthesis of ibotenic acid and X-ray analysis of an unexpected reaction product, (RS)-N-[2-(3-benzyloxyisoxazol-5-yl)-1-phenylethyl]-3-oxobutyramide

P. Krogsgaard‐Larsen, U. Madsen, L. Brehm, 1988 .

Regioselective lithiation and functionalization of 3-(benzyloxy)isothiazole: application to the synthesis of thioibotenic acid.

P. Krogsgaard‐Larsen, L. Bunch, U. Madsen, 2002, The Journal of organic chemistry.

Unprecedented migration of N-alkoxycarbonyl groups in protected pyroglutaminol.

P. Krogsgaard‐Larsen, L. Bunch, P. Norrby, 2001, Organic letters.

Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid.

P. Krogsgaard‐Larsen, H. Bräuner‐Osborne, U. Madsen, 1998, Journal of medicinal chemistry.

Mixed cyano-gilman cuprates: Advances in Conjugate addition to α, β-unsaturated pyroglutaminol

P. Krogsgaard‐Larsen, L. Bunch, U. Madsen, 2004 .

Mixed Cyano-Gilman Cuprates — Advances in Conjugate Addition to α,β-Unsaturated Pyroglutaminol.

P. Krogsgaard‐Larsen, L. Bunch, U. Madsen, 2002 .

Synthesis and pharmacological evaluation of novel conformationally constrained homologues of glutamic acid.

G. Roda, A. Pinto, L. Tamborini, 2007, European journal of medicinal chemistry.

Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.

E. Russo, G. De Sarro, P. Conti, 2003, Journal of medicinal chemistry.

Design of Cyclopentaisoxazoline Amino Acids as Conformationally Constrained Agonists at Glutamate Receptors

L. Toma, G. Roda, P. Conti, 2003 .

Design of novel conformationally restricted analogues of glutamic acid

G. Vistoli, L. Toma, G. Roda, 2003 .

Synthesis and pharmacology of a new AMPA-kainate receptor agonist with potent convulsant activity.

G. De Sarro, P. Conti, H. Bräuner‐Osborne, 1998, Journal of medicinal chemistry.

Design, synthesis, and pharmacological characterization of novel, potent NMDA receptor antagonists.

G. De Sarro, L. Toma, G. Roda, 2004, Journal of medicinal chemistry.

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).

T. Liljefors, A. Schousboe, J. Greenwood, 2003, Journal of medicinal chemistry.

Design of excitatory amino acid receptor agonists, partial agonists and antagonists: ibotenic acid as a key lead structure

P. Krogsgaard‐Larsen, H. Bräuner‐Osborne, U. Madsen, 1996 .

Resolution, absolute stereochemistry, and enantiopharmacology of the GluR1-4 and GluR5 antagonist 2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]propionic acid.

P. Krogsgaard‐Larsen, U. Madsen, J. Egebjerg, 1999, Chirality.

Novel 3‐Carboxy‐ and 3‐Phosphonopyrazoline Amino Acids as Potent and Selective NMDA Receptor Antagonists: Design, Synthesis, and Pharmacological Characterization

K. Hansen, A. Pinto, L. Tamborini, 2010, ChemMedChem.

Textbook of drug design and discovery

Tommy Liljefors, T. Liljefors, P. Krogsgaard‐Larsen, 2016 .

Ibotenic acid and thioibotenic acid: a remarkable difference in activity at group III metabotropic glutamate receptors.

J. Greenwood, P. Krogsgaard‐Larsen, C. Sánchez, 2004, European journal of pharmacology.

Novel class of amino acid antagonists at non-N-methyl-D-aspartic acid excitatory amino acid receptors. Synthesis, in vitro and in vivo pharmacology, and neuroprotection.

D. R. Curtis, P. Krogsgaard‐Larsen, N. Diemer, 1991, Journal of medicinal chemistry.

Tetrazolyl isoxazole amino acids as ionotropic glutamate receptor antagonists: synthesis, modelling and molecular pharmacology.

J. Greenwood, P. Krogsgaard‐Larsen, B. Frølund, 2005, Bioorganic & medicinal chemistry.

Pharmacology of AMPA/kainate receptors

P. Krogsgaard‐Larsen, U. Madsen, T. Stensbøl, 2001 .

Ionotropic excitatory amino acid receptor ligands. Synthesis and pharmacology of a new amino acid AMPA antagonist.

P. Krogsgaard‐Larsen, H. Bräuner‐Osborne, U. Madsen, 2000, European journal of medicinal chemistry.

Pharmacology and toxicology of ATOA, an AMPA receptor antagonist and a partial agonist at GluR5 receptors

A. Schousboe, P. Krogsgaard‐Larsen, P. Wahl, 1998, Neuropharmacology.

Antagonist properties of a phosphono isoxazole amino acid at glutamate R1-4 (R,S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid receptor subtypes.

P. Krogsgaard‐Larsen, S. Traynelis, P. Wahl, 1998, Molecular pharmacology.

Synthesis and pharmacology of highly selective carboxy and phosphono isoxazole amino acid AMPA receptor antagonists.

P. Krogsgaard‐Larsen, B. Bang-Andersen, U. Madsen, 1996, Journal of medicinal chemistry.

Modulation of AMPA receptor function in relation to glutamatergic abnormalities in Alzheimer's disease.

P. Krogsgaard‐Larsen, U. Madsen, B. Ebert, 1994, Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie.

Excitatory amino acid receptors: Multiplicity and ligand specificity of the NMDA and AMPA receptor subtypes

P. Krogsgaard‐Larsen, U. Madsen, B. Ebert, 1992 .

Novel Class of Amino Acid Antagonists at Non‐N‐methyl‐D‐aspartic Acid Excitatory Amino Acid Receptors. Synthesis, in vitro and in vivo Pharmacology, and Neuroprotection.

D. R. Curtis, P. Krogsgaard‐Larsen, N. Diemer, 1991 .

Synthesis of Novel N1‐Substituted Bicyclic Pyrazole Amino Acids and Evaluation of Their Interaction with Glutamate Receptors

G. Roda, A. Pinto, P. Conti, 2005, Chemistry & biodiversity.

Synthesis and pharmacology of 3-hydroxy-delta2-isoxazoline-cyclopentane analogues of glutamic acid.

L. Toma, P. Conti, H. Bräuner‐Osborne, 2002, Farmaco.

Different characteristics of AMPA receptor agonists acting at AMPA receptors expressed in Xenopus oocytes.

A. Schousboe, P. Krogsgaard‐Larsen, P. Wahl, 1996, European journal of pharmacology.

2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.

C. Mathiesen, E. Nielsen, A. Kristensen, 2003, Journal of medicinal chemistry.

Resolution, absolute stereochemistry and molecular pharmacology of the enantiomers of ATPA.

P. Krogsgaard‐Larsen, U. Madsen, B. Ebert, 1999, European journal of pharmacology.

NMDA receptor agonists derived from ibotenic acid. Preparation, neuroexcitation and neurotoxicity.

P. Krogsgaard‐Larsen, J. Ferkany, U. Madsen, 1990, European journal of pharmacology.

Rational design, synthesis, and pharmacological evaluation of 2-azanorbornane-3-exo,5-endo-dicarboxylic acid: a novel conformationally restricted glutamic acid analogue.

T. Liljefors, J. Greenwood, P. Krogsgaard‐Larsen, 2003, The Journal of organic chemistry.

Partial Agonism and Antagonism of the Ionotropic Glutamate Receptor iGLuR5

T. Liljefors, A. Schousboe, P. Naur, 2007, Journal of Biological Chemistry.

2-Amino-3-(3-hydroxy-1,2,5-thiadiazol-4-yl)propionic acid: resolution, absolute stereochemistry and enantiopharmacology at glutamate receptors.

P. Krogsgaard‐Larsen, H. Bräuner‐Osborne, K. Frydenvang, 2002, Bioorganic & medicinal chemistry.

Synthesis and receptor binding affinity of new selective GluR5 ligands.

T. H. Johansen, P. Krogsgaard‐Larsen, L. Bunch, 2001, Bioorganic & medicinal chemistry.

Cognitive enhancing effects of an AMPA receptor positive modulator on place learning in mice

Hana Malá, J. Mogensen, D. Pickering, 2012, Behavioural Brain Research.

Analogues of 3-Hydroxyisoxazole-Containing Glutamate Receptor Ligands Based on the 3-Hydroxypyrazole-Moiety: Design, Synthesis and Pharmacological Characterization

A. Kristensen, R. Clausen, D. Pickering, 2014, Neurochemical Research.

Design, synthesis and pharmacology of model compounds for indirect elucidation of the topography of AMPA receptor sites

P. Krogsgaard‐Larsen, B. Frølund, U. Madsen, 1993 .

Novel 1-hydroxyazole bioisosteres of glutamic acid. Synthesis, protolytic properties, and pharmacology.

J. Greenwood, P. Krogsgaard‐Larsen, S. Morel, 2002, Journal of Medicinal Chemistry.

Microsoft Word-72803376-file00

David E. Gloriam, J. M. Mathiesen, D. Gloriam, 2012 .

Analogues of 3-Hydroxyisoxazole-Containing Glutamate Receptor Ligands Based on the 3-Hydroxypyrazole-Moiety: Design, Synthesis and Pharmacological Characterization

A. Kristensen, R. Clausen, D. Pickering, 2014, Neurochemical Research.

New analogues of ACPD with selective activity for group II metabotropic glutamate receptors.

E. Mikiciuk-Olasik, H. Bräuner‐Osborne, U. Madsen, 1997, European journal of pharmacology.

Synthesis and biological activity of the N-alkyl derivatives of ibotenic acid

M. Dumpis, U. Madsen, L. B. Piotrovskii, 2006, Pharmaceutical Chemistry Journal.

Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA.

P. Krogsgaard‐Larsen, K. Frydenvang, U. Madsen, 2001, Chirality.

The AMPA receptor binding site: focus on agonists and competitive antagonists.

P. Krogsgaard‐Larsen, U. Madsen, T. Stensbøl, 2002, Current pharmaceutical design.

Studies of the antagonist actions of (RS)‐2‐amino‐3‐[5‐tert‐butyl‐3‐(phosphonomethoxy)‐4‐isoxazolyl]propionic acid (ATPO) on non‐NMDA receptors in cultured rat neurones

J. Lambert, U. Madsen, B. Ebert, 1998, British journal of pharmacology.

Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.

G. De Sarro, L. Toma, P. Conti, 1999, Journal of medicinal chemistry.

Glutamate receptor ligands: synthesis, stereochemistry, and enantiopharmacology of methylated 2-aminoadipic acid analogs.

P. Krogsgaard‐Larsen, H. Bräuner‐Osborne, K. Frydenvang, 2002, Chirality.

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.

P. Krogsgaard‐Larsen, K. Frydenvang, U. Madsen, 1996, Journal of medicinal chemistry.

Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to homoibotenic acid.

P. Krogsgaard‐Larsen, U. Madsen, B. Ebert, 1992, Journal of medicinal chemistry.

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

P. Krogsgaard‐Larsen, U. Madsen, B. Ebert, 1994, Neurochemistry International.

Excitatory amino acid receptor ligands: asymmetric synthesis, absolute stereochemistry and pharmacology of (R)- and (S)-homoibotenic acid.

P. Krogsgaard‐Larsen, U. Madsen, B. Ebert, 1995, Bioorganic & medicinal chemistry.