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Publications and patents

Book chapters

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. ISBN: 978-3-527-31456-0

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.


147. 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., online DOI

146. M. Ellwart, G. Höfner, A. Gerwien, K.T. Wanner, P. Knochel, Synthesis and Bioactivity of Novel N-Benzylic and N-Phenethylic Ephedrine Derivatives, Synthesis 2017 online DOI

145. T. Wein, G. Höfner, S. Rappenglück, S. Sichler, K.V. Niessen, T. Seeger, F. Worek, H. Thiermann, K.T. Wanner, Searching for putative binding sites of the bispyridinium compound MB327 in the nicotinic acetylcholine receptor, Tox. Lett. online DOI

144. K.V. Niessen, T. Seeger, S. Rappenglück, T. Wein, G. Höfner, K.T. Wanner, H. Thiermann, F. Worek: In vitro pharmacological characterization of the bispyridinium non-oxime compound MB327 and its 2- and 3-regioisomers, Tox. Lett. accepted.

143. K.V. Niessen, T. Seeger, S. Rappenglück, S. Sichler, T. Wein, C. Scheffel, G. Höfner, K.T. Wanner, F. Worek, H.Thiermann, Allosterische Modulation nikotinischer Acetylcholinrezeptoren - eine neue Therapieoption für die Behandlung von Nervenkampfstoffvergiftungen?, Wehrmedizinische Monatsschrift, 2017, 61, 5, 100-105.

142. M. Schaarschmidt, K.T. Wanner, "Synthesis of Allene Substituted Nipecotic Acids by Allenylation of Terminal Alkynes, J. Org. Chem, 2017, online DOI

141. M. Schuller, G. Höfner, K.T. Wanner, "Simultaneous Multiple MS Binding Assays addressing D1 and D2 Dopamine receptors", ChemMedChem 2017, accepted

140. S. Rappenglück, K.V. Niessen, T. Seeger, F. Worek, H. Thiermann, K.T. Wanner, "Regioselective and Transition Metal Free Addition of tertButyl Magnesium Reagents to Pyridine Derivatives – A Convenient Method for the Synthesis of 3-Substituted 4tert-Butylpyridine Derivatives", Synthesis 2017, 49, 4055-4064. DOI

139. 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 DOI

138. T. Lutz, T. Wein, G. Höfner, K.T. Wanner, "Development of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives with N-Arylalkynyl Substituents", ChemMedChem 2017, 12, 362-371. DOI

137. S. K. Schmidt, G. Höfner, K.T. Wanner, "Determination of enantiomeric excess of nipecotic acid as 1-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl) derivatives", Chirality 2017, 29, 48-56 DOI

136. K. Salat, A. Podkowa, N. Malikowska, F. Kern, J. Pabel, E. Wojcieszak, K. Kulig, K.T. Wanner, B. Strach, E. Wyska, "Novel, highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties", Neuropharmacology 2017, 113, 331-342. DOI

135. S. Kerscher-Hack, T. Renukappa-Gutke, G. Höfner, K.T. Wanner, "Synthesis and biological evaluation of a series of N-alkylated imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors", Eur. J. Med. Chem. 2016, 124, 852-880 DOI

134. 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. DOI

133. A. Sohail, K. Jayaraman, S. K. Venkatesan, K. Gotfryd, M. Daerr, U. Gether, C.J. Loland, K.T. Wanner, M. Freissmuth, W. Sandtner, T. Stockner, H. Sitte, "The environmental shapes the inner vestibule of LeuT", PLOS Computational Biology, 2016 DOI

132. T. Hellenbrand, G. Höfner, T. Wein, K.T. Wanner, "Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors", Bioorg. Med. Chem. 2016, 24, 2072-2096. (DOI)

131. T. Lutz, P. Spanner, K.T. Wanner, “A general approach to substituted diphenyldiazenes”, Tetrahedron 2016, online (DOI)

130. 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, in press

129. T. Wein, M. Petrera, L. Allmendinger, G. Höfner, J. Pabel, K. T. Wanner, "Different Binding Modes of Small and Large Binders of GAT1", ChemMedChem, 2016, 11, 509-518. (DOI).

128. M. Petrera, T. Wein, L. Allmendinger, M. Sindelar, J. Pabel, G. Höfner, K. T. Wanner, "Development of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives by Suzuki-Miyaura Cross-Coupling Reactions", ChemMedChem, 2015, 11, 519-538. (DOI)

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

126. S. Schmitt, G. Höfner, K.T. Wanner, "Application of MS Transport Assays to the Four Human γ-Aminobutyric Acid Transporters", ChemMedChem 2015, online (DOI)

125. S. 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. (DOI).

124. T. Steffan, T. Renukappa-Gutke, G. Höfner, K.T. Wanner, "Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-ylacetic acids", Bioorg. Med. Chem. 2015, 23, 1284-1306. (DOI)

123. A. Jakubowska, J. Pabel, M. Żylewski, K. T. Wanner, K. Kulig, "Asymmetric synthesis of all four stereoisomers of 1-amino-3-hydroxy-cyclopentanecarboxylic acid", Tetrahedron 2015, 71, 686-693. (DOI)

122. F. T. Kern, K.T. Wanner, "Generation and Screening of Oximes Libraries Addressing the Neuronal GABA Transporter GAT1", ChemMedChem. 2015, 10, 396-410. (DOI).

121. S.Grimm, G.Höfner, K.T. Wanner, "Development and validation of an LC-ESI-MS/MS method for the triple reuptake inhibitor Indatraline enabling its quantification in MS Binding Assays", Anal. Bioanal Chem 2015, 407, 471-485. (DOI).

120. S. Cuboni, C. Devigny, B. Hoogeland, A. Strasser, S. Pomplun, B. Hauger, G. Höfner, K.T. Wanner, M. Eder, A. Buschauer, F. Holsboer, F. Hausch, "Loratadine and analogs: Discovery and preliminary SAR of inhibitors of the amino acid transporter B0AT2", J. Med. Chem. 2014, 57, 9473-9479 (DOI).

119. L. Allmendinger, K.T. Wanner, Synthesis of [2H7] Indatraline, J. Labelled Compd. Radiopharm. 2014, 57, 721-724 (DOI).

118. G. Quandt, G. Höfner, J. Pabel, J. Dine, M. Eder, K. T. Wanner, "First Photoswitchable Neurotransmitter Transporter Inhibitor: Light-induced Control of γ-Aminobutyric Acid Transporter 1 (GAT1) Activity in Mouse Brain", J.Med. Chem. 2014, online (DOI)

117. 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, 7575-7583. (DOI)

116. P. Kowalczyk, K. Sałat, G. C. Höfner, M. Mucha, A. Rapacz, A. Podkowa, B. Filipek, K. T. Wanner, K. Kulig, "Synthesis, biological evaluation and structureeactivity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides", Eur. J. Med. Chem. 2014, 83, 256-273. (DOI)

115. 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)

114.T. Hellenbrand, K.T. Wanner, "Conjugate Addition of Organomagnesium Cuprates to Guvacine Derivatives", Eur. J. Org. Chem, 2014, 20, 4398-4409 [[http://dx.doi.org/10.1002/ejoc.201402259 | (DOI)]

113. C. Schmaunz, P. Mayer, K.T. Wanner, "Inter- and Intramolecular [4+2] Cycloaddition Reactions with 4,4-Disubstituted N-Silyl-1,4-Dihydropyridines as Precursors for N-Protonated 2-Azabutadiene Intermediates", Synthesis 2014, 46, 1630-1638. (DOI)

112. P. Kowalczyk, K. Sałat, G. C. Höfner, N. Guzior, B. Filipek, K. T. Wanner, K. Kulig, “2-Substituted 4-hydroxybutanamides as potential inhibitors of gamma-aminobutyric acid transporters mGAT1–mGAT4: Synthesis and biological evaluation, Bioorg. Med. Chem. 2013, 21, 5154-5167. (DOI)

111. 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).

110. 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)

109. I. Sitka, L. Allmendinger, G. Fülep, G. Höfner, K.T. Wanner, "Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors", Eur. J. Med. Chem., 2013, 65, 487-499. (DOI)

108. S. Petz, K. T. Wanner, "Synthesis of 3-Azabicyclo[3.2.0]heptane Derivatives as gamma-Aminobutyric Acid Analogues via Intermolecular [2+2] Photocycloaddition", Eur. J. Org. Chem, 2013, 19, 4017-4025. (DOI)

107. Cover Article 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)

106. M. Sindelar, T. A. Lutz, M. Petrera, K.T. Wanner, "Focused Pseudostatic Hydrazone Libraries Screened by Mass Spectrometry Binding Assay – Optimizing Affinities towards γ-Aminobutyric Acid Transporter 1", J. Med. Chem., 2013, 56, 1323-1340. (DOI)

105. X. Zhao, J. Pabel, G. Höfner, K.T. Wanner, "Synthesis and biological evaluation of 4- hydroxy-4-(4-methoxyphenyl)-substituted proline and pyrrolidin-2-ylacetic acid derivatives as GABA uptake inhibitors", Bioorg. Med. Chem., Bioorg. Med. Chem., 2013, 2, 470–484. (DOI)

104. 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)

103. K. Salat, A. Wieckowska, K. Wieckowski, G. Höfner, J. Kaminski, K. T. Wanner, B. Malawska, B. Filipek, K. Kulig, "Synthesis and pharmacological properties of new GABA uptake inhibitors", Pharmacol. Reports, 2012, 64, 817-833.

102. 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. (DOI)

101. Highlighted Paper in Nat. Chem. Biol. M. Sindelar, K.T. Wanner, "Library Screening by Means of MS Binding Assays - Exemplarily Demonstrated for a Pseudo-static Library Addressing GAT1", ChemMedChem, 2012, 7, 1678-1690. (DOI)

100. J. Pabel, M. Faust, C. Prehn, B. Wörlein, L. Allmendinger, G. Höfner, K. T. Wanner, "Development of a (S)-1-{2-[tris(4-methoxyphenyl)methoxy]ethyl}piperidine-3-carboxylic acid [(S)-SNAP-5114] carba analogue inhibitor for murine y- aminobutyric acid transporter type 4", ChemMedChem, online (DOI)

99. 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.

98. L. Iovkova-Berends, C. Wängler, T. Zöller, G. Höfner, K.T. Wanner, C. Rensch, P. Bartenstein, A. Kostikov, R. Schirrmacher, K. Jurkschat, B. Wängler, "t-Bu2SiF-Derivatized D2 -Receptor Ligands: The First SiFA-Containing Small Molecule Radiotracers for Target-Specific PET-Imaging, Molecules, 2011, 16, 7458-7479. (DOI)

97. C. Schmaunz, K.T. Wanner, "Synthesis of 4,4-Disubstituted Piperidine-2-carbonitriles and Piperidine-2,6-dicarbonitriles as Precursors for New 4,4-Disubstituted Pipecolic Acid and Piperidine-2,6-dicarboxylic Acid Derivatives", Synthesis, 2011, 20, 3332-3342. (DOI)

96. 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., 2011, 19, 6492-6504. (DOI)

95. Very Important Paper 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)

94. 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)

93. 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)

92. 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)

91. S. Michalakis, X. Zong, E. Becirovic, V. Hammelmann, T. Wein, K.T. Wanner, M. Biel, "The glutamic acid-rich protein is a gating inhibitor of cyclic nucleotide-gated channels", J. Neurosci., 2011, 31, 133-141. (DOI)

90. 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)

89. C. Wängler, D. Nada, G. Höfner, S. Maschauer, B. Wängler, S. Schneider, E. Schirrmacher, K.T. Wanner, R. Schirrmacher, O. Prante, "In vitro and initial in vivo evaluation of 68Ga-labeled transferrin receptor (TfR) binding peptides as potential carriers for enhanced drug transport into TfR expressing cells", Molecular Imaging & Biology, 2011, 13, 332-341. (DOI)

88. J. Bräckow, J. Pabel, P. Mayer, K. Polborn, K. T. Wanner, "Camphoric acid derived sulfur containing bicyclic carboxylic acids as chiral auxiliaries in N-acyliminium ion chemistry", Tetrahedron, 2010, 66, 7279-7287. (DOI)

87. C. Schmaunz, J. Pabel, K.T. Wanner, "Synthesis of 5-substituted 7,8-benzomorphans by intramolecular cyclizations of N-protected 4,4-disubstituted 1,4-dihydropyridines", Synthesis, 2010, 13, 2147-2160. (DOI)

86. 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. (DOI)

85. 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. (DOI)

84. T. Wein, K. T. Wanner, "Generation of a 3D model for human GABA transporter hGAT-1 using molecular modeling and investigation of the binding of GABA", J. Mol. Model, 2010, 16, 155-161. (DOI)

83. C. A. Sperger, P. Mayer, K.T. Wanner, "Application of an Ugi type reaction to a N-silyl-4,4-disubstituted 1,4-dihydropyridine", Tetrahedron, 2009, 65, 10463-10469. (DOI)

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

81. C. A. Sperger, K. T. Wanner, "Regioselective addition of organomagnesium reagents to N-silyl activated nicotinic acid esters - A convenient method for the synthesis of 4,4-disubstituted 1,4-dihydronicotinates", Tetrahedron, 2009, 65, 5824–5833. (DOI)

80. J. Pabel, E. Wadenstorfer, K.T. Wanner, "Asymmetric Synthesis of Pyridol[1,2-c]pyrimidones, Zeitschrift für Naturforschung B, 2009 (64b), 6, 653–661. (Link)

79. 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)

78. M. R. Faust, C. E. Hoesl, K. T. Wanner, 'Rearrangement of Dialkyl-2-(azetidin-3-yl)propane-1,3-dioates - A Structural Revision', Heterocycles, 2008, 75, 2981-2988. (DOI)

77. M. Ege, K. T. Wanner, "Diastereoselective synthesis of β-amino acid derivatives from dihydropyridones", Tetrahedron, 2008, 64, 7273-7282. (DOI)

76. S. Šimonyiová, K. T. Wanner, "Electrocyclic Ring-Opening Reactions may Cause Failure of Enolate Alkylation of 1,4-Oxazin-2-one Based Chiral Glycine Equivalents", Tetrahedron, 2008, 64, 5107-5110. (DOI)

75. 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)

74. 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)

73. E. S. Schremmer, K. T. Wanner, "Zinc Iodide as an Efficient Catalyst in the TMS-Azide Modified Passerini Reaction", Heterocycles, 2007, 74, 661-671. (DOI)

72. A. Müller, K. Polborn, K. T. Wanner, "Asymmetric Alkylation of N-Acylisoindolin-1-ones via α-Bromoimides: A Novel Route to 1-Substituted Isoindolines", J. Heterocyl. Chem., 2007, 44, 575-590. (DOI)

71. 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)

70. J. Bräckow, K. T. Wanner, "Direct Synthesis of 4,4-Disubstituted N-Silyl-1,4-Dihydropyridines", Tetrahedron, 2006, 62, 2395-2404. (DOI)

69. 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)

68. 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)

67. 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)

66. 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)

65. 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)

64. 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)

63. 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)

62. U. Weber, C. Hoesl, W. Ponikwar, M. Suter, H. Nöth, K. T. Wanner, "Stereoselective Synthesis of 1-Substituted 1,2,3,4-Tetra-hydro-β-carbolines by Asymmetric Electrophilic α-amidoalkylation Reactions", Heterocycles, 2004, 63, 2747-2767. (DOI)

61. M. Ege, K. T. Wanner, "Synthesis of β-Amino Acids based on Oxidative Cleavage of Dihydropyridone", Org. Lett., 2004, 6, 3553-3556. (DOI)

60. 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)

59. C. E. Hoesl, K. T. Wanner, "First Asymmetric Syntheses of 6-Substituted Nipecotic Acid Derivatives", Tetrahedron, 2004, 60, 307-318. (DOI)

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

57. M. Ludwig, K. Polborn, K. T. Wanner, “Asymmetric Synthesis of 1-Substituted 1,2,3,4-Tetrahydroisoquinolines by Asymmetric Electrophilic α-Amidoalkylation Reactions“, Heterocycles, 2003, 61, 299-326. (DOI)

56. R. Kammler, K. Polborn, K. T. Wanner, “Asymmetric Synthesis of a Tricyclic Core Structure of the Securinega Alkaloids Virosecurinine and Allosecurinine”, Tetrahedron, 2003, 59, 3359–3368. (DOI)

55. 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)

54. C.-J. Koch, S. Šimonyiová, J. Pabel, A. Kärtner, K. Polborn, K. T. Wanner, “Asymmetric Synthesis with 6-tert-Butyl-5-methoxy-6-methyl-3,6-dihydro-2H-1,4-oxazin-2-one as a New Chiral Glycine Equivalent: Preparation of Enantiomerically Pure α-Tertiary and α-Quaternary α-Amino Acids”, Eur. J. Org. Chem., 2003, 1244-1263. (DOI)

53. C. E. Hoesl, J. Pabel, K. Polborn, K. T. Wanner, „Synthesis of Sterically Demanding 3-Silylpyridines and their Use in Asymmetric Synthesis with Chiral N-Acyliminium Ions“, Heterocycles, 2002, 58, 383 – 392. (DOI)

52. C. E. Hoesl, M. Maurus, J. Pabel, K. Polborn, K. T. Wanner, “Generation of Chiral N-Acylpyridinium Ions by Means of Silyl Triflates and their Diastereoselective Trapping Reaction: Formation of N-Acyldihydropyridines and N-Acyldihydropyridones”, Tetrahedron, 2002, 58, 6757–6770. (DOI)

51. J. Pabel, C. E. Hösl, M. Maurus, M. Ege, K. T. Wanner, "Generation of N-Acylpyridinium Ions from Pivaloyl Chloride and Pyridine Derivatives by Means of Silyl Triflates", J. Org. Chem., 2000, 65, 9272-9275. (DOI)

50. 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. (DOI)

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

48. O. Achatz, A. Grandl, K. T. Wanner, "Asymmetric Synthesis Employing a Chiral 5-Methoxy-1,4-oxazin-2-one Derivative: Preparation of Enantiomerically Pure α-Quaternary α-Amino Acids.", Eur. J. Org. Chem., 1999, 1967-1978. (DOI)

47. C. E. Hösl, K. T. Wanner, "Syntheses of 4-Silyl-substituted Methyl Nicotinates via Silylcupration of N-Acylpyridinium Salts", Heterocycles, 1998, 48, 2653-2659. (DOI)

46. 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. (DOI)

45. 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.

44. 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. (DOI)

43. M. Ludwig, H. Beer, H. Lotter, K. T. Wanner, "The Absolute Configuration of (1S)-(+)- and (1R)-(-)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline. A Revision of the Literature Assignment.", Tetrahedron: Asymmetry, 1997, 8, 2693-2695. (DOI)

42. 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. (DOI)

41. K. T. Wanner, U. Weber, "A Convenient Synthesis of 1,3-Oxazolidin 4-ones and 1,3 Oxazine-4-ones", J. Heterocycl. Chem., 1997, 34 , 681-683. (DOI)

40. 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. (DOI)

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

38. K. T. Wanner, F. Paintner, "Asymmetrische Elektrophile α-Amidoalkylierung-11: Neue chirale Hilfsgruppen aus (+)-Camphersäure", Liebigs Ann., 1996, 1941-1948. (DOI)

37. 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. (DOI)

36. U. Weber, K. T. Wanner, "Einstufige Synthese von Oxazolo[3',2':1,2]pyrido[3,4-b]indolen durch direkte Kondensationsreaktionen von 3,4-Dihydro-β-carbolin mit α-Hydroxy-α-butyrolactonen", Zeitschrift f. Naturforschung, 1995, 50b, 677-680.

35. F. Eiden, E. Reimann, H.-D. Stachel, H. Wagner, K. T. Wanner, M. H. Zenk, "Zusammenraufen oder auseinandersetzen.", PZ, 1995, 140, 2568-2570.

34. F. Eiden, E. Reimann, H.-D. Stachel, H. Wagner, K. T. Wanner, M. H. Zenk, "Anleitung zum Ruinieren eines angesehenen Berufsstandes", PZ, 1995, 140, 1108-1111.

33. K. T. Wanner, F. Paintner, "Asymmetric Electrophilic α-Amidoalkylation (AEaA), 10: A New Camphorimide Derived Chiral Auxiliary for the Asymmetric Synthesis with N-Acyliminium Ions - Preparation of Aracemic 2-Substituted Piperidines", Tetrahedron, 1994, 50, 3113-3122. (DOI)

32. K. T. Wanner, U. Weber, "Oxazolo[3',2':1,2]pyrido[3,4 b]indole und [1,3]-Oxazino[3',2':1,2]pyrido[3,4-b]indole durch eine einfache Kondensationsreaktion von 3,4- Dihydro-β-carbolin mit α- bzw. β-Hydroxycarbonsäuren, Synthesis,1994, 4, 387-390. (DOI)

31. K. T. Wanner, "Chiral N-acyliminium ions as new tools in the asymmetric synthesis of CNS-active compounds", Eur. J. Pharm. Sci., 1994, 2,62-64. (DOI)

30. K. T. Wanner, St. Stamenitis, "Asymmetrische Synthesen mit chiralen 1,4-Oxazin-2,5-dionen: Darstellung enantiomerenreiner 2-substituierter Pipecolinsäurederivate", Liebigs Ann. Chem., 1993, 477-484. (DOI)

29. K. T. Wanner, C. Wolf, "Elektrophile α-Amidoalkylierung mit Enamiden nach einem neuen Aktivierungsverfahren mit O,O´ Dimethyldithiophosphorsäure", Arch. Pharm., 1993, 326, 799-802. (DOI)

28. K. T. Wanner, E.Wadenstorfer, A. Kärtner, "Asymmetric Electrophilic Amidoalkylation, 9: Highly Stereoselective Syntheses of 2-Substituted Piperidines", Synlett, 1991, 797-799. (DOI)

27. 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. (DOI)

26. 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. (DOI)

25. 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. (DOI)

24. K. T. Wanner, I. Praschak, U. Nagel, "Asymmetric Electrophilic α-Amidoalkylation 7: Generation, Chrystal Structure and Trapping Reactions of a Chiral 6,7-Dimethoxy-1,2,3,4-tetra-hydroisoquinoline Derived N-Acyliminium Ion", Arch. Pharm., 1990, 323, 335-350. (DOI)

23. K. T. Wanner, I. Praschak, "Asymmetric Electrophilic α-Amidoalkylation 6: Syntheses of Tetrahydroisoquinolines of High Enantiomeric Purity", Heterocycles, 1989, 29, 29-33.(DOI)

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

21. 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. (DOI)

20. K. T. Wanner, A. Kärtner, "Neue chirale Hilfsgruppen: Herstellung optisch aktiver Cyclopentancarbonsäuren aus (-)-Camphansäure", Synthesis, 1988, 968-970. (DOI)

19. K. T. Wanner, A. Kärtner, E. Wadenstorfer,"Asymmetric Electrophilic α-Amidoalkylation 5: Improved Stereoselectivities Through New Chiral Auxiliaries", Heterocycles, 1988, 27, 2549-2556. (DOI)

18. K. T. Wanner, "Neue chirale Hilfsgruppen: Gewinnung einer phenylazaanalogen Camphansäure nach veränderter N/O-Regioselektivität einer Ringverengungsreaktion", Liebigs Ann. Chem., 1988, 603-604. (DOI)

17. K. T. Wanner, "Synthesen und Ringverengungsreaktionen α-halogenierter N-Phenylcamphersäureimide", Arch. Pharm., 1988, 321, 353-356. (DOI)

16. K. T. Wanner, "Tetrahydro-3-pyranon: Die Regioselektivität bei der Bildung reaktiver Intermediate", Arch. Pharm., 1988, 321, 81-83. (DOI)

15. K. T. Wanner, A. Kärtner, "Asymmetrische α-Amidoalkylierung. Synthesen enantiomerenreiner, α-substituierter Piperidine mit 1-Camphanoyl-1,2,3,4 tetrahydropyridin", Arch. Pharm., 1987, 320, 1253-1267.

14. K. T. Wanner, A. Kärtner, "Pd/C-katalysierte Doppelbindungisomerisierung von N-Acylallylaminen zu N-Acylenaminen", Arch. Pharm., 1987, 320, 1050-1058.

13. K. T. Wanner, J. Schünemann, "Synthesen optisch aktiver Oxazolo [3,2-a]piperidine via Enamide", Arch. Pharm., 1987, 320, 1161-1167.

12. K. T. Wanner, A. Kärtner, "Asymmetric α-Amidoalkylation. Synthesis of α-Substituted Piperidines of High Enantiomeric Purity", Heterocycles, 1987, 26, 921-924. (DOI)

11. K. T. Wanner, A. Kärtner, "Isomerization of N-Acyl-1,2,5,6 Tetrahydropyridines to N-Acylenamines by Palladium on Carbon", Heterocycles, 1987, 26, 917-919. (DOI)

10. A. I. Meyers, B. A. Lefker, K. T. Wanner, R. A. Aitken, "An Asymmetric Synthesis of Chiral 4,4-Disubstituted Cyclohexanones in High Enantiomeric Purity", J. Org. Chem., 1986, 51, 19361938. (DOI)

9. A. I. Meyers, R. Hanreich, K. T. Wanner, "Efficient Asymmetric Synthesis of (+)-Mesembrine and Related Chiral 4,4-Disubstituted Cylohexanones", J. Am. Chem. Soc., 1985,107, 7776-7778. (DOI)

8. A. I. Meyers, K. T. Wanner, "Chiral Quaternary Carbon Compounds, II. An Asymmetric Synthesis of (R) or (S)-4,4-Dialkyl-2-Cyclopentenones", Tetrahedron Lett., 1985, 26, 2047-2050. (DOI)

7. K. T. Wanner, A. Kärtner, "Cyclobutanon-Enamine: Synthese und Reaktionen des (1-Cyclobutenyl)piperidins", Arch. Pharm., 1985, 318, 655-658. (DOI)

6. F. Eiden, W. Winkler, K. T. Wanner, A. Markhauser, "Zentralwirksame 4- Phenylpyrane: Hydrierte Phenylchromene, Phenylaza- und Phenyloxachromene sowie Phenyloxa- und Phenyldioxaxanthene durch [4+2]-Cycloaddition", Arch. Pharm., 1985, 318, 648-655. (DOI)

5. F. Eiden, K. T. Wanner, "5,6-Dihydro-2-H-pyran-3(4H)-on als Baustein zur Synthese pyrananellierter Heterocyclen", Liebigs Ann. Chem., 1984, 1759-1777. (DOI)

4. F. Eiden, K. T. Wanner, "Pyrano- und Naphthopyrano[3,2-b]indol Derivate", Arch. Pharm., 1985, 318, 648-655. (DOI)

3. F. Eiden, K. T. Wanner, "Regiospezifische Synthese von 2 Phenylpyrano-[3,4-b]pyranonen (Oxaflavon-Derivaten) mit Tetrahydro-3-pyranon", Arch. Pharm., 1985, 318, 207-209. (DOI)

2. K. T. Wanner, F. Eiden, "Benzothiazole durch C-C-Spaltung von α-[(2-Nitrophenyl)-thio]ketonen", Liebigs Ann. Chem., 1984, 1100-1108. (DOI)

1. F. Eiden, K. T. Wanner, "Tetrahydro-3-pyranon als Baustein zur Pyrano[3,2-b]pyran- Synthese", Arch. Pharm., 1984, 317, 958-962. (DOI)



3. Wanner, Klaus; Höfner, Georg; Bertling, Wolf; Kosak, Hans. “Method for the determining the binding behaviour of ligands which specifically bind to target molecules”. PCT Int. Appl. (2002), 44 pp. CODEN: PIXXD2 WO 2002095403 A2 20021128.

2. Wanner, Klaus; Höfner, Georg; Bertling, Wolf. “Method for determining the quantity of ligands that are bound to target molecules.“ PCT Int. Appl. (2001), 39 pp. CODEN: PIXXD2 WO 2001094943 A2 20011213 .

1. Wanner, Klaus; Fuelep, Guenther; Höfner, Georg. “GABA-uptake-Inhibitoren mit Pyrrolidinstruktur”. Ger. Offen. (2000), 36 pp. CODEN: GWXXBX DE 19840611 A1 20000309.

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