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Harald Hübner

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Cornelia Held; Harald Hübner; Ralf Kling; Yvonne A Nagel; Helma Wennemers; Peter Gmeiner
Impact of the Proline Residue on Ligand Binding of Neurotensin Receptor 2 (NTS2)-Selective Peptide-Peptoid Hybrids.
Fabrizio Sanna; Nuska Tschammer; Harald Hübner; Stefan Löber; Birgit Ortner; Peter Gmeiner
Discovery of dopamine D₄ receptor antagonists with planar chirality.
Cornelia Held; Harald Hübner; Jasmin Meltretter; Monika Pischetsrieder; Manuel Plomer; Peter Gmeiner
Development of a metabolically stable neurotensin receptor 2 (NTS2) ligand.

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All Publications

2013: Cornelia Held; Harald Hübner; Ralf Kling; Yvonne A Nagel; Helma Wennemers; Peter Gmeiner
Impact of the Proline Residue on Ligand Binding of Neurotensin Receptor 2 (NTS2)-Selective Peptide-Peptoid Hybrids.
ChemMedChem 2013;8(5):772-8.
2013: Fabrizio Sanna; Nuska Tschammer; Harald Hübner; Stefan Löber; Birgit Ortner; Peter Gmeiner
Discovery of dopamine D₄ receptor antagonists with planar chirality.
Bioorganic & medicinal chemistry 2013;21(7):1680-4.
2013: Cornelia Held; Harald Hübner; Jasmin Meltretter; Monika Pischetsrieder; Manuel Plomer; Peter Gmeiner
Development of a metabolically stable neurotensin receptor 2 (NTS2) ligand.
ChemMedChem 2013;8(1):75-81.
2012: Stefan Löber; Maria Rosaria Melis; Fabrizio Sanna; Antonio Argiolas; Armin Buschauer; Harald Hübner; Peter Gmeiner
Novel azulene derivatives for the treatment of erectile dysfunction.
Bioorganic & medicinal chemistry letters 2012;22(23):7151-4.
2011: Julia Kühhorn; Dawn Thompson; Jennifer Whistler; Andreas W Götz; Harald Hübner; Peter Gmeiner
Development of a bivalent dopamine D₂ receptor agonist.
Journal of medicinal chemistry 2011;54(22):7911-9.
2011: Julia Kühhorn; Harald Hübner; Peter Gmeiner
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.
Journal of medicinal chemistry 2011;54(13):4896-903.
2011: Alexandra Kekewska; Peter Gmeiner; Harald Hübner; Heinz H Pertz
The bulky N6 substituent of cabergoline is responsible for agonism of this drug at 5-hydroxytryptamine 5-HT2A and 5-HT2B receptors and thus is a determinant of valvular heart disease.
The Journal of pharmacology and experimental therapeutics 2011;338(1):381-91.
2011: Gerald Pratsch; Johannes F Unfried; Jürgen Einsiedel; Manuel Plomer; Harald Hübner; Peter Gmeiner; Markus R Heinrich
Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand.
Organic & biomolecular chemistry 2011;9(10):3746-52.
2011: Jürgen Einsiedel; Cornelia Held; Maud Hervet; Harald Hübner; Manuel Plomer; Nuska Tschammer; Peter Gmeiner
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
Journal of medicinal chemistry 2011;54(8):2915-23.
2011: Nuska Tschammer; Jan Elsner; Angela Goetz; Katharina Ehrlich; Stefan Schuster; Miriam Ruberg; Julia Kühhorn; Dawn Thompson; Jennifer Whistler; Harald Hübner; Peter Gmeiner
Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions.
Journal of medicinal chemistry 2011;54(7):2477-91.
2011: Stefan Löber; Harald Hübner; Nuska Tschammer; Peter Gmeiner
Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates.
Trends in pharmacological sciences 2011;32(3):148-57.
2010: S B Höfling; Simone Maschauer; Harald Hübner; Peter Gmeiner; Hans-Jürgen Wester; Olaf Prante; M R Heinrich
Synthesis, biological evaluation and radiolabelling by 18F-fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET.
Bioorganic & medicinal chemistry letters 2010;20(23):6933-7.
2010: Stefan Bollinger; Harald Hübner; Frank W Heinemann; Karsten Meyer; Peter Gmeiner
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
Journal of medicinal chemistry 2010;53(19):7167-79.
2010: Marika Skultety; Harald Hübner; Stefan Löber; Peter Gmeiner
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
Journal of medicinal chemistry 2010;53(19):7219-28.
2010: Carsten Hocke; Simone Maschauer; Harald Hübner; Stefan Löber; Wolfgang Utz; Torsten Kuwert; Peter Gmeiner; Olaf Prante
A series of 18F-labelled pyridinylphenyl amides as subtype-selective radioligands for the dopamine D3 receptor.
ChemMedChem 2010;5(6):941-8.
2010: Nuska Tschammer; Harald Hübner; Miriam Dörfler; Peter Gmeiner
Engineering a GPCR-ligand pair that simulates the activation of D(2L) by Dopamine.
ACS chemical neuroscience 2010;1(1):25-35.
2010: Simone Maschauer; Jürgen Einsiedel; Roland Haubner; Carsten Hocke; Matthias Ocker; Harald Hübner; Torsten Kuwert; Peter Gmeiner; Olaf Prante
Labeling and glycosylation of peptides using click chemistry: a general approach to (18)F-glycopeptides as effective imaging probes for positron emission tomography.
Angewandte Chemie (International ed. in English) 2010;49(5):976-9.
2009: Daniela Huber; Harald Hübner; Peter Gmeiner
1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands.
Journal of medicinal chemistry 2009;52(21):6860-70.
2009: Katharina Ehrlich; Andreas W Götz; Stefan Bollinger; Nuska Tschammer; Laura Bettinetti; Steffen Härterich; Harald Hübner; Harald Lanig; Peter Gmeiner
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
Journal of medicinal chemistry 2009;52(15):4923-35.
2009: Pilar Rodriguez Loaiza; Stefan Löber; Harald Hübner; Peter Gmeiner
Parallel synthesis of potent dopaminergic N-phenyltriazole carboxamides applying a novel click chemistry based phenol linker.
Bioorganic & medicinal chemistry 2009;17(15):5482-7.
2009: Sabine Linz; Jörg Müller; Harald Hübner; Peter Gmeiner; Reinhard Troschütz
Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.
Bioorganic & medicinal chemistry 2009;17(13):4448-58.
2009: Stefan Löber; Nuska Tschammer; Harald Hübner; Maria Rosaria Melis; Antonio Argiolas; Peter Gmeiner
The azulene framework as a novel arene bioisostere: design of potent dopamine D4 receptor ligands inducing penile erection.
ChemMedChem 2009;4(3):325-8.
2008: Miriam Dörfler; Nuska Tschammer; Katharina Hamperl; Harald Hübner; Peter Gmeiner
Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.
Journal of medicinal chemistry 2008;51(21):6829-38.
2008: Carsten Hocke; Olaf Prante; Ismael Salama; Harald Hübner; Stefan Löber; Torsten Kuwert; Peter Gmeiner
18F-Labeled FAUC 346 and BP 897 derivatives as subtype-selective potential PET radioligands for the dopamine D3 receptor.
ChemMedChem 2008;3(5):788-93.
2008: Olaf Prante; Rainer Tietze; Carsten Hocke; Stefan Löber; Harald Hübner; Torsten Kuwert; Peter Gmeiner
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
Journal of medicinal chemistry 2008;51(6):1800-10.
2008: Jürgen Einsiedel; Harald Hübner; Maud Hervet; Steffen Härterich; Susanne Koschatzky; Peter Gmeiner
Peptide backbone modifications on the C-terminal hexapeptide of neurotensin.
Bioorganic & medicinal chemistry letters 2008;18(6):2013-8.
2008: Tilo Görnemann; Harald Hübner; Peter Gmeiner; Reinhard Horowski; Klaus Peter Latté; Miroslav Flieger; Heinz H Pertz
Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A receptors.
The Journal of pharmacology and experimental therapeutics 2008;324(3):1136-45.
2008: Rainer Tietze; Stefan Löber; Harald Hübner; Peter Gmeiner; Torsten Kuwert; Olaf Prante
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
Bioorganic & medicinal chemistry letters 2008;18(3):983-8.
2007: Pilar Rodriguez Loaiza; Stefan Löber; Harald Hübner; Peter Gmeiner
Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes.
Bioorganic & medicinal chemistry 2007;15(23):7248-57.
2007: Daniela Stark; Markus Piel; Harald Hübner; Peter Gmeiner; Gerhard Gründer; Frank Rösch
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
Bioorganic & medicinal chemistry 2007;15(21):6819-29.
2007: Ismail Salama; Carsten Hocke; Wolfgang Utz; Olaf Prante; Frank Boeckler; Harald Hübner; Torsten Kuwert; Peter Gmeiner
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
Journal of medicinal chemistry 2007;50(3):489-500.
2006: Ismail Salama; Karin Schlotter; Wolfgang Utz; Harald Hübner; Peter Gmeiner; Frank Boeckler
CoMFA and CoMSIA investigations of dopamine D3 receptor ligands leading to the prediction, synthesis, and evaluation of rigidized FAUC 365 analogues.
Bioorganic & medicinal chemistry 2006;14(17):5898-912.
2006: Cécile Enguehard-Gueiffier; Harald Hübner; Ahmed El Hakmaoui; Hassan Allouchi; Peter Gmeiner; Antonio Argiolas; Maria Rosaria Melis; Alain Gueiffier
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.
Journal of medicinal chemistry 2006;49(13):3938-47.
2006: Karin Schlotter; Frank Boeckler; Harald Hübner; Peter Gmeiner
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.
Journal of medicinal chemistry 2006;49(12):3628-35.
2006: Stefan Löber; Harald Hübner; Peter Gmeiner
Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.
Bioorganic & medicinal chemistry letters 2006;16(11):2955-9.
2006: Pilar Rodriguez Loaiza; Stefan Löber; Harald Hübner; Peter Gmeiner
Click chemistry on solid phase: parallel synthesis of N-benzyltriazole carboxamides as super-potent G-protein coupled receptor ligands.
Journal of combinatorial chemistry 2006;8(2):252-61.
2006: Olaf Prante; Carsten Hocke; Stefan Löber; Harald Hübner; Peter Gmeiner; Torsten Kuwert
Tissue distribution of radioiodinated FAUC113: assessment of a pyrazolo(1,5-a) pyridine based dopamine D4 receptor radioligand candidate.
Nuklearmedizin. Nuclear medicine 2006;45(1):41-8.
2005: Carsten Hocke; Olaf Prante; Stefan Löber; Harald Hübner; Peter Gmeiner; Torsten Kuwert
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents.
Bioorganic & medicinal chemistry letters 2005;15(21):4819-23.
2005: Jan Elsner; Frank Boeckler; Frank W Heinemann; Harald Hübner; Peter Gmeiner
Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists.
Journal of medicinal chemistry 2005;48(18):5771-9.
2005: Carola Lenz; Frank Boeckler; Harald Hübner; Peter Gmeiner
Fancy bioisosteres: synthesis, SAR, and pharmacological investigations of novel nonaromatic dopamine D3 receptor ligands.
Bioorganic & medicinal chemistry 2005;13(14):4434-42.
2005: Karin Schlotter; Frank Boeckler; Harald Hübner; Peter Gmeiner
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.
Journal of medicinal chemistry 2005;48(11):3696-9.
2005: Laura Bettinetti; Harald Hübner; Peter Gmeiner
Chirospecific and subtype selective dopamine receptor binding of heterocyclic methoxynaphthamide analogs.
Archiv der Pharmazie 2005;338(5-6):276-80.
2005: Frank Boeckler; Ursula Ohnmacht; Thomas Lehmann; Wolfgang Utz; Harald Hübner; Peter Gmeiner
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.
Journal of medicinal chemistry 2005;48(7):2493-508.
2005: Laura Bettinetti; Stefan Löber; Harald Hübner; Peter Gmeiner
Parallel synthesis and biological screening of dopamine receptor ligands taking advantage of a click chemistry based BAL linker.
Journal of combinatorial chemistry 2005;7(2):309-16.
2005: Carola Lenz; Christian Haubmann; Harald Hübner; Frank Boeckler; Peter Gmeiner
Fancy bioisosteres: synthesis and dopaminergic properties of the endiyne FAUC 88 as a novel non-aromatic D3 agonist.
Bioorganic & medicinal chemistry 2005;13(1):185-91.
2004: Holger Bittermann; Jürgen Einsiedel; Harald Hübner; Peter Gmeiner
Evaluation of lactam-bridged neurotensin analogues adjusting psi(Pro10) close to the experimentally derived bioactive conformation of NT(8-13).
Journal of medicinal chemistry 2004;47(22):5587-90.
2004: Carsten Hocke; Olaf Prante; Stefan Löber; Harald Hübner; Peter Gmeiner; Torsten Kuwert
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.
Bioorganic & medicinal chemistry letters 2004;14(15):3963-6.
2004: Frank Boeckler; Holger Russig; Weining Zhang; Stefan Löber; John A Schetz; Harald Hübner; Boris Ferger; Peter Gmeiner; Joram Feldon
FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia.
Psychopharmacology 2004;175(1):7-17.
2004: Thomas Hussenether; Harald Hübner; Peter Gmeiner; Reinhard Troschütz
Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: synthesis and biological testing.
Bioorganic & medicinal chemistry 2004;12(10):2625-37.
2004: Carola Lenz; Frank Boeckler; Harald Hübner; Peter Gmeiner
Analogues of FAUC 73 revealing new insights into the structural requirements of nonaromatic dopamine D3 receptor agonists.
Bioorganic & medicinal chemistry 2004;12(1):113-7.
2003: Jürgen Einsiedel; Klaus Weber; Christoph Thomas; Thomas Lehmann; Harald Hübner; Peter Gmeiner
Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid.
Bioorganic & medicinal chemistry letters 2003;13(19):3293-6.
2003: Jürgen Einsiedel; Harald Hübner; Peter Gmeiner
Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312.
Bioorganic & medicinal chemistry letters 2003;13(5):851-4.
2002: Laura Bettinetti; Karin Schlotter; Harald Hübner; Peter Gmeiner
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.
Journal of medicinal chemistry 2002;45(21):4594-7.
2002: Stefan Löber; Harald Hübner; Peter Gmeiner
Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725.
Bioorganic & medicinal chemistry letters 2002;12(17):2377-80.
2002: Markus Bergauer; Harald Hübner; Peter Gmeiner
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.
Bioorganic & medicinal chemistry letters 2002;12(15):1937-40.
2002: Annette Moll; Harald Hübner; Peter Gmeiner; Reinhard Troschütz
Phenylpiperazinylmethylindolecarboxylates and derivatives as selective D(4)-ligands.
Bioorganic & medicinal chemistry 2002;10(6):1671-9.
2002: Stefan Löber; Tarek Aboul-Fadl; Harald Hübner; Peter Gmeiner
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.
Bioorganic & medicinal chemistry letters 2002;12(4):633-6.
2001: Thomas Lehmann; Harald Hübner; Peter Gmeiner
Dopaminergic 7-aminotetrahydroindolizines: ex-chiral pool synthesis and preferential D3 receptor binding.
Bioorganic & medicinal chemistry letters 2001;11(21):2863-6.
2001: Jürgen Einsiedel; Harald Hübner; Peter Gmeiner
Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179).
Bioorganic & medicinal chemistry letters 2001;11(18):2533-6.
2001: Stefan Löber; Harald Hübner; Wolfgang Utz; Peter Gmeiner
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
Journal of medicinal chemistry 2001;44(17):2691-4.
2000: Harald Hübner; J Kraxner; Peter Gmeiner
Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.
Journal of medicinal chemistry 2000;43(23):4563-9.
2000: Jürgen Einsiedel; Christoph Thomas; Harald Hübner; Peter Gmeiner
Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.
Bioorganic & medicinal chemistry letters 2000;10(17):2041-4.
2000: J Kraxner; Harald Hübner; Peter Gmeiner
Azepino- and diazepinoindoles: synthesis and dopamine receptor binding profiles.
Archiv der Pharmazie 2000;333(9):287-92.
2000: Harald Hübner; Christian Haubmann; Wolfgang Utz; Peter Gmeiner
Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.
Journal of medicinal chemistry 2000;43(4):756-62.
1999: Christian Haubmann; Harald Hübner; Peter Gmeiner
Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.
Bioorganic & medicinal chemistry letters 1999;9(21):3143-6.
1999: Christian Haubmann; Harald Hübner; Peter Gmeiner
2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.
Bioorganic & medicinal chemistry letters 1999;9(14):1969-72.
1999: Christoph Thomas; Harald Hübner; Peter Gmeiner
Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.
Bioorganic & medicinal chemistry letters 1999;9(6):841-6.
1999: Stefan Löber; Harald Hübner; Peter Gmeiner
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.
Bioorganic & medicinal chemistry letters 1999;9(1):97-102.
1996: H Achenbach; Harald Hübner; M Reiter
Cholestane- and pregnane-type glycosides from the roots of Tribulus cistoides.
Phytochemistry 1996;41(3):907-17.
1996: H Achenbach; Harald Hübner; M Reiter
New cardioactive steroid saponins and other glycosides from Mexican Tribulus cistoides.
Advances in experimental medicine and biology 1996;404():357-70.
1995: H Achenbach; Harald Hübner; W Vierling; W Brandt; M Reiter
Spiganthine, the cardioactive principle of Spigelia anthelmia.
Journal of natural products 1995;58(7):1092-6.
1994: H Achenbach; Harald Hübner; W Brandt; M Reiter
Cardioactive steroid saponins and other constituents from the aerial parts of Tribulus cistoides.
Phytochemistry 1994;35(6):1527-43.