Group of Prof. Daniel Merk - Faculty for Chemistry and Pharmacy

Dr. Georg Höfner

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

Zi.Nr.: C1.060
Tel.: +49 (0)89 2180 77277
Fax.: +49 (0)89 2180 77247


LC-MS Analytik | Projektleiter und Beauftragter für biologsche Sicherheit in gentechnischen Anlagen | Strahlenschutzbeauftragter


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


G.Höfner, K.T.Wanner, MS Binding Assays in: J. Kool, W. M.A. Niessen (Hrsg.), Analyzing Biomolecular Interactions by Mass Spectrometry (Wiley-VHC Weinheim 2015), 165-198.

G. Höfner, C. Zepperitz, K. T. Wanner, 'MS Binding Assays - An Alternative to Radioligand Binding', in: K. T. Wanner, G. Höfner (Hrsg.), Mass Spectrometry in Medicinal Chemistry (Wiley-VHC, Weinheim, 2007), 247-283.

ausgewählte Publikationen

S. Nayak, D. Joseph, G. Höfner, A. Dakua, A.Athreya, K. Wanner, B. Kanner, A. Penmatsa, "Cryo-EM structure of GABA transporter 1 reveals substrate recognition and transport mechanism", Nat. Struct. Mol. Biol., 2023 accepted

M. Währa, L. allmendinger, G. Höfner, K.T. Wanner, "Benocyclidine (BTCP) as non-labelled reporter ligand for MS Binding Assays for the PCP ion channel binding site of  the desensitized Torpedo nicotinic acetylcholine
receptor (nAChR)", ChemMedChem, 2023, in press

H. Kipka,  R.Tomasi, M. Hübner, U. Liebchen, C. Hagl, K.T. Wanner, H. Mannell, G. Höfner, "Simultaneous LC-ESI-MS/MS Quantification of Levosimendan and Its Metabolites for Therapeutic Drug Monitoring of Cardiac Surgery Patients", Pharmaceutics 2022, 14, 1454 (

T.M. Ackermann, G. Höfner, K.T. Wanner, "Screening for New Inhibitors of Glycine Transporter 1 and 2 by Means of MS Binding Assays", ChemMedChem, 2021, 16, 1-12

T.M. Ackermann, L. Allmendinger, G. Höfner, K.T. Wanner, "MS Binding Assays for Glycine Transporter 2 (GlyT2)", ChemMedChem, 2020, 15, 1-18

J.Gabriel, G. Höfner, K.T. Wanner, "A Library Screening Strategy Combining the Concepts of MS Binding Assays and Affinity Selection Mass Spectrometry", Frontiers in Chemistry, 2019, 7

T. M. Ackermann, K. Bhokare, G. Höfner, K.T. Wanner, MS binding assays for GlyT1 based on Org24598 as nonlabelled reporter ligand, Neuropharmacology 2019, 161, 107561

T. J. Hauke, T. Wein, G. Höfner, K.T. Wanner, Novel Allosteric Ligands of γ‑Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries, J. Med. Chem., 2018, 61, 10310–10332

P. Neiens, A. De Simone, G. Höfner, K. T. Wanner, Simultaneous Multiple MS Binding Assays for the dopamine, the norepinephrine, and the serotonin transporter, ChemMedChem, 2018, 13, 453-463

S. Sichler, G. Höfner, S. Rappenglück, T. Wein, K. V. Niessen, T. Seeger, F. Worek, H. Thiermann, F. F. Paintner, K. T. Wanner, Development of MS Binding Assays targeting the binding site of MB327 at the nicotinic acetylcholine receptor, Tox. Lett., 2018, 293, 172-183.

M. Schuller, G. Höfner, K.T. Wanner, "Simultaneous Multiple MS Binding Assays addressing D1 and D2 Dopamine receptors", ChemMedChem 2017, 2017, 12, 1585-1594.

P. Neiens, G. Höfner, K. T. Wanner, "Determination of the enantiomeric purity of the selective dopamin transporter inhibitor (+)-R-R-4-(2-benzhydryloxyethyl)-1-(4-fluorbenzyl)piperidin-3-ol", Chirality 2017, 29, 294-303.

G. Cattaneo, D. Ubiali, E. Calleri, M. Rabuffetti, G. Höfner, K.T. Wanner, M.C. De Morares, L. K. B. Martinelli, D. S. Santos, G. Speranza, G. Massolini, "Development, validation and application of a 96-well enzymatic assay based on LC-ESI-MS/MS quantification for the screening of selective inhibitors against Mycobacterium tuberculosis purine nucleoside phosphorylase", Analytica Chimica Acta 2016, 943, 89-97.

T. Kirmeier, R. Gopalakrishnan, V. Ganal, A.M. Werner, S. Cuboni, G. C. Rudolf, G. Höfner, K.T. Wanner, S.A. Sieber, F. Holsboer, T. Rein, F. Hausch, "Azidobupramine, a novel chemical probe to enlighten antidepressants' mode of action", PLOS one, 2016

P. Neiens, G. Höfner, K.T. Wanner, "MS Binding Assays for D₁ and D₅ Dopamine Receptors", ChemMedChem, 2015, 10, 1924-1931.

S. Schmitt, G. Höfner, K.T. Wanner, "Application of MS Transport Assays to the Four Human γ-Aminobutyric Acid Transporters", ChemMedChem 2015, 10, 1498-1510.

S. H. Grimm, G. Höfner, K.T. Wanner, "MS Binding Assays for the three Monoamine Transporters Employing the Triple Reuptake Inhibitor (1R,3S)-Indatraline as Native Marker", ChemMedChem, 2015, 10, 1027-1039.

S. Schmitt, G. Höfner, K.T. Wanner, MS Transport Assays for γ-aminobutyric acid transporters – an efficient alternative for radiometric assays, Anal Chem, 2014, 86 (15), 7575–7583. (DOI)

C. Wängler, S. Chowdhury, G. Höfner, P. Djurova, E.O. Purisima, P. Bartenstein, B. Wängler, G. Fricker, K.T. Wanner, R. Schirrmacher, Shuttle−Cargo Fusion Molecules of Transport Peptides and the hD2/3 Receptor Antagonist Fallypride: A Feasible Approach To Preserve Ligand−Receptor Binding?. J. Med. Chem. 2014, 57, 4368-4381. (DOI)

S. Schiesser, T. Pfaffeneder, K. Sadeghian, B. Hackner, B. Steigenberger, A.S. Schröder, J. Steinbacher, G. Kashiwazaki, G. Höfner, K.T. Wanner, C. Ochsenfeld, T. Carell, “Deamination, Oxidation and C-C bond Cleavage Reactivity of 5-Hydroxymethylcytosine, 5-Formylcytosine and 5-Carboxycytosine”, J. Am. Chem. Soc. 2013, 135, 14593-14599. (DOI)

S. Grimm, L. Allmendinger, G. Höfner, K.T. Wanner,”Enantiopurity Determination of the Enantiomers of the Triple Reuptake Inhibitor Indatraline”, Chirality, 2013, '25'', 923-933. (DOI)

G. Quandt, G. Höfner, K. T. Wanner, "Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors, Bioorg. Med. Chem. 2013, 21, 3363-3378. (DOI)

M. Polley, G. Höfner, K.T. Wanner, "Development and validation of an LC-ESI-MS/MS quantification method for a potential γ-aminobutyric acid transporter 3 (GAT3) marker and its application in preliminary MS binding assays", Biomed. Chromatogr., 2013, 27, 641-654. (DOI)

Y. Zhou, S. Holmseth, C. Guo, B. Hassel, G. Höfner, H.S. Huitfeldt, K.T. Wanner, N.C. Danbolt, "Deletion of the GABA transporter 2 (GAT2, SLC6A13) gene in mice leads to changes in liver and brain taurine contents", J. Biol. Chem., 2012, 287, 35733-35746.

P. Kowalczyk, G. Höfner, K.T. Wanner, K. Kulig, "Synthesis And Pharmacological Evaluation Of New 4,4-Diphenylbut-3-Enyl Derivatives Of 4-Hydroxybutanamides As Gaba Uptake Inhibitor", Acta Poloniae Pharmaceutica, 2012, 69, 157-160.

M. Hess, G. Höfner, K.T. Wanner, "(S)- and (R)-Fluoxetine as Native Markers in MS Binding Assays Addressing the Serotonin Transporter", ChemMedChem, 2011 , 6, 1900-1908. (DOI)

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", Bioorg. Med.Chem. Lett., 2011, 21, 5795-5799. (DOI)

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, 2011, 400, 3505-3515. (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)

G. Höfner, K. T. Wanner, "Kompetitive Bindungsstudien leicht gemacht - mit nativem Marker und massenspektrometrischer Quantifizierung", Angew. Chem., 2003, 115, 5393-5395 (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.

G. Höfner and B. Schmidt, Species differences in [3H]linopirdine (DUP 996) binding to brain membranes, Eur. J. Pharmacol, 298, 307-312, 1996.

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.