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Dr. Georg Höfner

Department Pharmazie
- Zentrum für Pharmaforschung -
Ludwig-Maximilians-Universität München
Butenandtstraße 7
D-81377 München

Zi.Nr.: C2.082
Tel.: +49 (0)89 2180 77277
Fax.: +49 (0)89 2180 77247
Mail: Georg.Hoefner@cup.uni-muenchen.de




Area of responsibilty

Biological Screening

Dissertation

Asymmetrische Synthesen ZNS-wirksamer 2-(2-Pyrolidinyl)ethanole mit chiralen α-Amidoalkylierungsreagenzien

Publications

E. Schaffert, G. Höfner, K.T. Wanner, "Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1–mGAT4: Synthesis and biological evaluation", Bioorg. Med. Chem., submited

M. Hess, G. Höfner, K.T. Wanner, "(S)- and (R)-Fluoxetine as Native Markers in MS Binding Assays Addressing the Serotonin Transporter", ChemMedChem, submitted

A. Müller, G. Höfner, T. Renukappa-Gutke, C. Parsons, K.T. Wanner, "Synthesis of a series of γ-amino alcohols comprising a N-methyl isoindoline moiety and their evaluation as NMDA receptor antagonists", ChemMedChem, submitted

M. Hess, G. Höfner, K.T. Wanner, "Development and validation of a rapid LC-ESI-MS/MS method for quantification of fluoxetine and its application to binding assays", Anal. Bioanal. Chem, online (DOI)

S. Hack, B. Wörlein, G. Höfner, J. Pabel, K.T. Wanner, "Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors", Eur. J. Med. Chem., 2011, 46, 1483-1498. (DOI)

K. Kulig, A. Więckowska, K. Więckowski, J. Gajda, B. Pochwat, G. Höfner, K.T. Wanner, B. Malawska, "Synthesis and biological evaluation of new derivatives of 2-substituted 4-hydroxybutanamides as GABA uptake inhibitors", Eur. J. Med. Chem., 2011, 46, 183-190. (DOI)

M. R. Faust, G. Höfner, J. Pabel, K. T. Wanner; "Azetidine Derivatives as Novel GABA Uptake Inhibitors: Synthesis, Biological Evaluation, and Structure-Activity Relationship", Eur. J. Med Chem, 2010, 45, 2453-2466.

G. Höfner, K. T. Wanner, "Using short columns to speed up LC-MS quantification in MS binding assay", J. Chromatogr., B, 2010, 878, 1356-1364.

G. Höfner, D. Merkel, K. T. Wanner, "MS binding assays - with MALDI towards high throughput", ChemMedChem, 2009, 4, 1523-1528. (DOI)

D. Hui, K. N. Kumar, J. R. Mach, A. Srinivasan, R. Pal, X. Bao, A. Agbas, G. Höfner, K. T. Wanner, E. K. Michaelis, "A rat brain bicistronic gene with an internal ribosome entry site codes for phencyclidine binding protein with cytotoxic activity", JBC, 2009, 284, 2245-2257. (DOI)

C. Zepperitz, G. Höfner, K. T. Wanner, "Expanding the Scope of MS Binding Assays to Low Affinity Markers as Exemplified for mGAT1", Anal. Bioanal. Chem., 2008, 391, 309-316. (DOI)

A. Kragler, G. Höfner, K. T. Wanner, "Synthesis of Aminomehtylphenol Derivatives as Inhibitors of the Murine GABA Transporters mGAT1-mGAT4", Eur. J. Med. Chem., 2008, 43, 2404-2411. (DOI)


M. Ludwig, C. E. Hoesl, G. Höfner, K. T. Wanner, "Affinity of 1-aryl-1,2,3,4-tetrahydroisoquinoline derivatives to the ion channel binding site of the NMDA receptor complex", Eur. J. Med. Chem., 2006, 41, 1003-1010. (DOI)

G. H. Fülep, C. E. Hoesl, G. Höfner, K. T. Wanner, "New highly potent GABA uptake inhibitors selective for GAT-1 and GAT-3 derived from (R)- and (S)-proline and homologous pyrrolidine-2-alkanoic acids", Eur. J. Med. Chem., 2006, 41, 809-824. (DOI)

C. Zepperitz, G. Höfner, K. T. Wanner, "MS-Binding assays: kinetic, saturation and competitive experiments based on quantitation of bound marker – exemplified by the GABA transporter mGAT1", ChemMedChem, 2006, 1, 208-217.''' (DOI)


U. Meyer, P. Bisel, H. Braeuner-Osborne, U. Madsen, G. Höfner, K. T. Wanner, A. W. Frahm, "Rigid nonproteinogenic cyclic amino acids as ligands for glutamate receptors: trans-tris(homoglutamic) acids", Chirality, 2005, 17, 99-107. (DOI)

K. V. Niessen, G. Höfner, K. T. Wanner, "Competitive MS binding assays for Dopamine D2 receptors employing spiperone as a native marker", ChemBioChem, 2005, 6, 1769 – 1775. (DOI)


A. Kragler, G. Höfner, K. T. Wanner, "Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4", Eur. J. Pharmacol., 2005, 519, 43-47. (DOI)


G. Höfner, C. E. Hoesl, C. Parsons,G. Quack, K. T. Wanner, "NMDA-NR2B subtype selectivity of stereoisomeric 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives", Bioorg. Med. Chem. Lett., 2005, 15, 2231-2234. (DOI)


X. Zhao, C. Hoesl, G. Höfner, K. T. Wanner, "Synthesis and Biological Evaluation of New GABA Uptake Inhibitors Derived from Proline and from Pyrrolidine-2-acetic Acid", Eur.J. Med.Chem., 2005, 40, 231-247. (DOI)


G. Höfner, K. T. Wanner, "Evaluation of GABA Uptake in Subcellular Fractions of Bovine Frontal Cortex and Brain Stem", Neurosci. Lett., 2004, 364, 53-57. (DOI)

C.-J. Koch, G. Höfner, K. Polborn, K. T. Wanner,“Synthesis of the Four Stereoisomers of 1-Amino-2-(hydroxymethyl)cyclobutanecarboxylic Acid and Their Biological Evaluation as Ligands for the Glycine Binding Site of the NMDA Receptor“, Eur. J. Org. Chem., 2003, 2233-2242. (DOI)

J. Pabel, G. Höfner, K. T. Wanner, "Synthesis and Resolution of Racemic Eliprodil and Evaluation of the Enantiomers of Eliprodil as NMDA Receptor Antagonists.", Bioorg. Med. Chem. Lett., 2000, 10, 1377-1380.

G. Höfner, K. T. Wanner, "[3H]Ifenprodil Binding to NMDA-Receptors in Porcine Hippocampal Brain Membranes.", Eur. J. Pharmacol., 2000, 394, 211-219.

K. T. Wanner, H. Beer, G. Höfner, M. Ludwig, "Asymmetric Synthesis and Enantioselectivity of Binding of 1-Aryl-1,2,3,4-Tetrahydroisoquinolines at the PCP Site of the NMDA-Receptor Complex.", Eur. J. Org. Chem., 1998, 2019-2029.


I. Stroetmann, G. Seitz, K. T. Wanner, G. Höfner, "Syntheses of Novel Pyrazolomorphinans and their Binding to µ- and κ-Opioid-Receptors.", Pharmazie, 1998, 53, 87-90.

Th. Klindert, I. Stroetmann, G. Seitz, G. Höfner, K. T. Wanner, G. Frenzen und B. Eckhoff, "Syntheses of Novel Pyridazinomorphinans by Inverse Electron Demand Cycloaddition and their Binding to µ and κ Receptors.", Arch. Pharm. Pharm. Med. Chem., 1997, 330, 163-168.

G. Höfner, K. T. Wanner, "Characterisation of the binding of [3H]MDL 105,519, a radiolabelled antagonist for the N-methyl-D-Aspartate-associated glycine site, to pig cortical brain membranes", Neurosci. Lett., 1997, 226, 79-82.

G. Höfner, K. T. Wanner, "Characterisation of [3H]MK-801 binding and its cooperative modulation by pig brain membranes", J. of Recept. Signal Transduction Research, 1996, 16 (5&6), 297-313.


K. Görlitzer, I.-M. Weltroski, K. T. Wanner, G. Höfner, "Mannich-Basen von Morphinen, Isomorphinen und Chlormorphiden", Scientia Pharmaceutica, 1996, 64, 391-398.

K. T. Wanner, I. Praschak, G. Höfner, H. Beer, "Asymmetric Synthesis and Enantiospecifity of Binding of 2-(1,2,3,4-Tetrahydro-1-isoquinolyl)-ethanol-Derivatives to m and k Receptors", Arch. Pharm., 1996, 329, 11-22.

K. T. Wanner, G.Höfner, "Chelat- und Nicht-Chelat kontrollierte Reduktionen von β-Amidoketonen: Synthese nicht-racemischer 1,3-Aminoalkohole mit Pyrrolidinstruktur", Tetrahedron, 1991, 47, 1895-1910.

K. T. Wanner, G. Höfner, "Konfigurationsbestimmung von (2S,7aR)-und (2S,7aS)-2- Benzyl-5,6,7,7α -tetrahydropyrrolo[2,1-b]oxazol-3(2H)-on", Arch.Pharm., 1991, 324,191-193.


K. T. Wanner, G. Höfner, "Asymmetrische Elektrophile α-Amidoalkylierung 8: Gewinnung optisch aktiver α-Phenacylpyrrolidinamide und erste asymmetrische Totalsynthese des Norruspolins", Arch. Pharm., 1990, 323, 977-986.

K. T. Wanner, G. Höfner, "Asymmetrische Elektrophile α-Amidoalkylierung 4: Erzeugung und Abfangreaktionen chiraler N-Acylpyrrolidiniumionen", Arch. Pharm., 1989, 322, 99-103.


K. T. Wanner, G. Höfner, "Asymmetrische Elektrophile α-Amidoalkylierung 3: Synthesen von Vorstufen für die Erzeugung chiraler N-Acylpyrrolidiniumionen", Arch. Pharm., 1989, 322, 93-97.

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