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aktuell - 2006        2005 - 2001        2000 und früher

          2010

  1. K. Sander, Y. von Coburg, J.-C. Camelin, X. Ligneau, O. Rau, M. Schubert-Zsilavecz, J.-C. Schwartz, and H. Stark.
    Acidic Elements in Histamine H3 Receptor Antagonists.
    Bioorg. Med. Chem. Lett. 2010, 20, 1581-1584.

  2. M. Geschwandtner, K. Rossbach, W. Bäumer, M. Kietzmann, D. Dijkstra, H. Stark, T. Werfel, and R. Gutzmer.
    Murine and Human La    ngerhans Cells Express a Functional Histamine H4 Receptor: Modulation of Cell Migration and Function.
    Allergy, in press.

  3. K. Sander, T. Kottke, E. Proschak, Y. Tanrikulu, E. H. Schneider, R. Seifert, G. Schneider, and H. Stark.
    Lead Identification and Optimization of Diaminopyrimidines as Histamine H4 Receptor Ligands.
    Inflamm. Res. 2010, 59 (Suppl.), S249 – S251.

  4. K. J. Kuder, T. Kottke, H. Stark, X. Ligneau, J.-C. Camelin, R. Seifert, and K. Kieć- Kononowicz.
    Search for Novel, Highly Affine Histamine H3 Receptor Ligands with Fluorescent Properties.
    Inflamm. Res.     2010, 59 (Suppl.), S247 – S248.






    2009

  1. K. Roßbach, S. Wendorff, K. Sander, H. Stark, R. Gutzmer, T. Werfel, M. Kietzmann, and W. Bäumer.
    Histamine H4 Receptor Antagonism Reduces Hapten-Induced Scratching Behaviour but not Inflammation.
    Exp. Dermatol. 2009, 18, 57-63.

  2. E. Proschak, K. Sander, H. Zettl, Y. Tanrikulu, O. Rau, P. Schneider, M. Schubert-Zsilavecz, H. Stark and G. Schneider.
    From Molecular Shape to Potent Bioactive Agents II: Fragment-Based de novo Design.
    ChemMedChem 2009, 4, 45-48.

  3. K. J. Kuder, X. Ligneau, J.-C. Camelin, D. Lazeska, J.-C. Schwartz, W. Schunack, H. Stark, and K. Kiec-Kononowiecz.
    Diether (    Substituted)piperidine Derivatives as Novel Active Histamine H3 Receptor Ligands.
    Inflamm. Res. 2009, 58 (Suppl. 1), S47-S48.

  4. R. Gutzmer, S. Mommert, M. Gschwandtner, K. Zwingmann, H. Stark, and T. Werfel.
    The Histamine H4 Receptor is Functionally Expressed on Th2 Cells.
    J. Allergy Clin. Invest. 2009, 123, 619-625.

  5. Y. von Coburg, T. Kottke, L. Weizel, X. Ligneau, and H. Stark.
    Potential Utility of Histamine H3 Receptor Antagonist Pharmacophore in Antipsychotics.
    Bioorg.     Med. Chem. Lett. 2009, 19, 538-542.

  6. K. Roßbach, H. Stark, K. Sander, R. Leurs, M. Kietzmann, and W. Bäumer.
    The Histamine H4 Receptor as a New Target for Treatment of Canine Inflammatory Skin Disease.
    Vet. Dermatol. 2009, 20, 555-561.

  7. D. Lazewska, K. Kuder, X. Ligneau, J.-C. Camelin, W. Schunack, H. Stark, and K. Kiec-Kononowicz.
    Diether Derivatives of Homo- or Substituted Piperidines as Non-Imidazole Histamine H3 Receptor Ligands.
    Bioorg. Med. Chem. 2009, 17, 3037-42.

  8. Y. Tanrikulu, E. Proschak, T. Werner, T. Geppert, N. Todoroff, A. Klenner, T. Kottke, K. Sander, E. Schneider, R. Seifert, H. Stark, T. Clark, and G. Schneider.
    Homology Model Adjustment and Ligand Screening with a Pseudoreceptor of the Human Histamine H4 Receptor.
    ChemMedChem 2009, 4, 820-827.
    ChemMedChem 2009, 4, 694 (inside cover).

  9. A. Berthet, G. Porras, E. Doudnikoff, H. Stark, M. Cador, E. Bezard, and B. Bloch.
    Pharmacological Analysis Demonstrates Dramatic Alteration of D1 Dopamine Receptor Neuronal Distribution in the Rat Analog of L-DOPA-Induced Dyskinesia.
    J. Neurosci. 2009, 29, 4829-4835.

  10. K. Isensee, M. Amon, A. Garlaparti, X. Ligneau, J.-C. Camelin, M. Capet, J.-C. Schwartz, and H. Stark.
    Fluorinated Non-Imidazole Histamine H3 Receptor Antagonists.
    Bioorg. Med. Chem.     Lett. 2009, 19, 2172-2175; Erratum 2009, 19, 3348.

  11. E. Tiligada, E. Zampeli, K. Sander, and H. Stark.
    Investigational Agents for Targeting Histamine H3 and H4 Receptors.
    Expert Opin. Investig. Drugs 2009, 18, 1519-1531.

  12. K. Sander, T. Kottke, E. Proschak, Y. Tanrikulu, L. Weizel, E. H. Schneider, R. Seifert, G. Schneider, and H. Stark.
    Diaminopyrimidines as Histamine H4 Receptor Ligands – Lead Structure Identification by Virtual Screening and Scaffold Optimization.
    Bioorg. Med. Chem. 2009, 17, 7186-7196.

  13. D. Łażewska, M. Więcek, X. Ligneau, T. Kottke, L. Weizel, R. Seifert, W. Schunack, H. Stark, and K. Kieć-Kononowicz.
    Histamine H3 and H4 Receptor Affinity of Branched 3-(1H-Imidazol-4-yl)propyl N-alkylcarbamates.
    Bioorg. Med. Chem. Lett. 2009, 19, 6682-6685.







          2008

  1. D. Dijkstra, H. Stark, P. L. Chazot, F. C. Shenton, R. Leurs, T. Werfel, and R. Gutzmer.
    Human Inflammatory Dendritic Epidermal Cells Express a Functional Histamine H4 Receptor.
    J. Invest. Dermatol. 2008, 128, 1696-1703.

  2. D. Lazewska, K. Kuder, X. Ligneau, J.-C. Schwartz, W. Schunack, H. Stark, and K. Kiec-Kononowicz.
    Piperidine Variations in Search for Non-Imidazole Histamine H3 Receptor Ligands.
    Bioorg. Med. Chem. 2008, 16, 8729-8736.

  3. W. Bäumer, S. Wendorff, R. Gutzmer, T. Werfel, D. Dijkstra, P. Chazot, F. C. Shenton, H. Stark, and M. Kietzmann.
    Histamine H    4 Receptors Modulate Dendritic Cell Migration through Skin – Immunomodulatory Role of Histamine.
    Allergy 2008, 63, 1387-1394.

  4. N. Levoin, T. Calmels, O. Poupardin-Olivier, O. Labeeuw, D. Danvy, P. Robert, I. Berrebi-Bertrand, C.R. Ganellin, W. Schunack, H. Stark, and M. Capet.
    Refined Docking as a Valuable Tool for Lead Optimization: Application to Histamine H3 Receptor Antagonists.
    Arch. Pharm. 2008, 341, 610-623.

  5. K. Sander, T. Kottke, and H. Stark.
    Histamine H3 Receptor Antagonists Go to Clinics.
    Biol. Pharm.     Bull. 2008, 31, 2163-2181.

  6. K. Sander, H. Zettl, M. Schubert-Zsilavecz und H. Stark.
    Medizinische Chemie von Antitussiva und Expektorantien.
    Pharm. Unse    rer Zeit 2008, 37, 462-471; Erratum 2009, 38, 11.

  7. D. Marcinello, S. Ferré, V. Casado, A. Cortés, B. Le Foll, C. Mazzola, F. Drago, O. Saur, H. Stark, A. Soriano, C. Barnes, S. R. Goldberg, C. Lluis, K. Fuxe, and R. Franco.
    Identification of Dopamine D1-D3 Receptor Heteromers: Indications for a Role of Synergistic D1-D3 Receptor Interactions in the Striatum.
    J. Biol.     Chem. 2008, 283, 26016-26025.

  8. M. Jean, J. Renault, J.-C. Camelin, N. Levoin, D. Danvy, H. Stark, M. Capet, and P. Uriac.
    A Solid Phase Parallel Synthesis of Diverse Amides as Dopamine D3 Receptor Ligands.
    J. Enzym. Inhib. Med. Chem. 2008, 23, 588-592.






    2007

  1. X. Ligneau, D. Perrin, L. Landais, J.-C. Camelin, T. P. G. Calmels, I. Berrebi-Bertrand, J.-M. Lecomte, R. Parmentier, C. Anaclet, J.-S. Lin, V. Bertaina-Anglade, C. Drieu la Rochelle, F. d´Aniello, A. Rouleau, F. Gbahou, J.-M. Arrang, C. R. Ganellin, H. Stark, W. Schunack, and J.-C. Schwartz.
    BF2.649, a Non-Imidazole Inverse Agonist/Antagonist at the Human Histamine H3 Receptor: Preclinical Pharmacology.
    J. Pharmacol. Exp. Ther. 2007, 320, 365-375.

  2. H. Kubas und H. Stark.
    Klassische Wirkstoffentwicklung: Medizinische Chemie von Histamin-H2-Rezeptorantagonisten.
    Pharm. unserer Zeit 2007, 36, 24-32.

  3. B. C. Sasse, U. R. Mach, J. Leppaenen, T. Calmels, and H. Stark.
    Hybrid Approach for the Design of Highly Affine and Selective Dopamine D3 Receptor Ligands using Privileged Scaffolds of Biogenic Amine GPCR Ligands.
    Bioorg. Med. Chem. 2007, 15, 7258-7273.

  4. M. Amon, X. Ligneau, J.-C. Camelin, I. Berrebi-Bertrand, J.-C. Schwartz, and H. Stark.
    Highly Potent Fluorescence-Tagged Nonimidazole Histamine H3 Receptor Ligands.
    ChemMedChem 2007, 2, 708-716.

  5. O. Saur, A. E. Hackling, S. Perachon, J.-C. Schwartz, P. Sokoloff, and H. Stark.
    N-(4-(4-(2-Halogenophenyl)piperazin-1-yl)butyl)cinnamoyl Amide Derivatives as Dopamine D2 and D3 Receptor Ligands.
    Arch. Pharm. Chem. Life Sci. 2007, 340, 178-184.

  6. D. Dijkstra, R. Leurs, P. Chazot, F. Shenton, H. Stark, T. Werfel, and R. Gutzmer.
    Histamine Down-Regulates Monocyte CCL2 Production via the Histamine H4 Receptor.
    J. Allergy Clin. Immunol. 2007, 120, 300-307.

  7. B. Schlegel, C. Laggner, T. Langer, D. Schnell, R. Seifert, H. Stark, H.-D. Höltje, and W. Sippl.
    Generation of a Homology Model of the Human Histamine H3 Receptor for Ligand Docking and Pharmacophore-based Screening.
    J. Comput. Aided Mol. Des. 2007, 21, 437-453.

  8. A. Böcker, B. C. Sasse, M. Nietert, H. Stark, and G. Schneider.
    GPCR Targeted Library Design: Novel Dopamine D3 Receptor Antagonists.
    ChemMedChem 2007, 2. 1000-1005.

  9. K. Isensee, G. Petroianu, and H. Stark.
    Pharmacological Aspects of Cognitive Impairment: Past, Present, and Future of Drugs in Dementia.
    J. Appl. Biosci. 2007, 5, 57-70.






    2006

  1. G. Petrianou, K. Arafat, B. C. Sasse and H. Stark
    Multiple Enzyme Inhibitions of Histamine H3 Receptor Antagonists as Potential Procognitive Agents.
    Pharmazie 2006, 61, 179-182.

  2. D. Łażewska, X. Ligneau, J.-C. Schwartz, W. Schunack, H. Stark and K. Kieć-Kononowicz.
    Ether Derivatives of 3-Piperidinopropan-1-ol as Non-Imidazole Histamine H3 Receptor Antagonists.
    Bioorg. Med. Chem. 2006, 14, 3522-3529.

  3. M. Amon, X. Ligneau, J.-C. Schwartz and H. Stark
    Fluorescent Non-imidazole Histamine H3 Receptor Ligands with Nanomolar Affinities.
    Bioorg. Med. Chem. Lett. 2006, 16, 1938-1940.

  4. T. Noeske, B. C. Sasse, H. Stark, C. G. Parsons, T. Weil and G. Schneider
    Predicting Compound Selectivity by Self-Organizing Maps: Cross-Activities of Metabotropic Glutamate Receptor Antagonists.
    ChemMedChem 2006, 1,1066-1068.






    2005

  1. B. Le Foll, P. Sokoloff, H. Stark and S. R. Goldberg
    Dopamine D3 Receptor Ligands Block Nicotine-Induced Conditioned Place Preferences Through a Mechanism that Does Not Involve Discriminative-Stimulus or Antidepressant-Like Effects.
    Neuropsychopharmacology 2005, 30, 720-730.

  2. J. Apelt, S. Graßmann, X. Ligneau, C. R. Ganellin, J.-M. Arrang, J.-C. Schwartz, W. Schunack and H. Stark
    Search for Histamine H3 Receptor Antagonists with Combined Inhibitory Potency at N-Methyltransferase: Ether Derivatives.
    Pharmazie 2005, 60, 97-106.

  3. A. Lozada, M. Maegele, H. Stark, E. M. Neugebauer and P. Panula
    Traumatic Brain Injury Results in Mast Cell Increase and Changes in Regulation of Central Histamine Receptors.
    Neuropathol. Appl. Neurobiol. 2005, 31, 150-162.

  4. B. Schlegel, W. Sippl, H. Stark and H.-D. Höltje
    Model of a Specific hH3-Receptor Binding Pocket Suitable for Virtual Drug Design.
    Inflamm. Res. 2005, 54 (Suppl. 1), S50-S51.

  5. P. Heidler, V. Zohrabi-Kalantari, M. Capet, T. Calmels, J.-C. Schwartz, H. Stark and A. Link
    Parallel Synthesis and D    opamine D2/3 Receptor Affinities of N-{4-[4-(2-Methoxyphenyl)piperazin-1-yl]butyl}carboxamides.
    Bioorg. Med. Chem. 2005, 13, 2009-2014.

  6. D. Łażewska, K. Kieć-Kononowicz, S. Elz, H. H. Pertz, H. Stark and W. Schunack
    Piperidine-Containing Histamine H3 Receptor Antagonists of the Carbamate Class: The Alkyl Derivatives.
    Pharmazie 2005, 60, 403-410.

  7. E. Byvatov, B. C. Sasse, H. Stark and G. Schneider
    From Virtual to Real Screening for Dopamine D3 Receptor Ligands.
    ChemBioChem 2005, 6, 997-999.

  8. C. Guigoni, I. Aubert, Q. Li, V. V. Gurech, J. L. Benovic, S. Ferry, U. Mach, H. Stark. L. Leriche, K. Hakansson, B. H. Bioulac, C. E. Gross, P. Sokoloff, G. Fisone, E. V. Gurevich, B. Bloch and E. Bezard
    Pathogenesis of Levodopa-Induced Dyskinesia: Focus on D1 and D3 Dopamine Receptors.
    Parkinsonism Rel. Disord. 2005, 11 (Suppl. 1), S25-S29.

  9. R. Gutzmer, C. Diestel, S. Mommert, B. Köther, H. Stark, M. Wittmann and T. Werfel
    Histamine H4 Receptor Stimulation Suppress IL-12p70 Production and Mediates Chemotaxis in Human Monocyte-Derived Dendritic Cells.
    J. Immunol. 2005, 174, 5224-5232.

  10. M. Schubert-Zsilavecz und H. Stark
    Strukturen, Mechanismen und Entwicklungen: Protonenpumpeninhibitoren.
    [Proton Pump Inhibitors.]
    Pharm. unserer Zeit 2005, 34, 194-199.

  11. H. Stark, Y. Syha, L. Popescu und M. Schubert-Zsilavecz
    Innovationen in der Pipeline: Neue Wirkstoffe zur GERD-Behandlung.
    [New Drugs for GERD Treatment.]
    Pharm. unsere Zeit 2005, 34, 224-227.

  12. H. Stark und M. Schubert-Zsilavecz
    Medizinische Chemie der L-Typ-Calcium-Kanalblocker.
    [The Medicinal Chemistry of L-Type Calcium Channel Blockers.]
    Pharm. unserer Zeit 2005, 34, 374-379.






    2004

  1. U. R. Mach, A. E. Hackling, S. Perachon, S. Ferry, C. G. Wermuth, J.-C. Schwartz, P. Sokoloff and H. Stark
    Development of Novel 1,2,3,4-Tetrahydroisoquinoline Derivatives and Closely Related Compounds as Potent and Selective Dopamine D3 Receptor Ligands.
    ChemBioChem 2004, 5, 508-518.

  2. H. Stark und M. Schubert-Zsilavecz
    Entwicklungen, Strukturen und neue Tendenzen: H1-Antihistaminika.
    [Development, Structures and New Trends: H1-Antihistamines.]
    Pharm. unserer Zeit 2004, 33 (2), 92-98.

  3. O. Guillin, N. Griffon, J. Diaz, B. LeFoll, E. Bezard, C. Gross, C. Lammers, H. Stark, P. Carroll, J.-C. Schwartz and P. Sokoloff
    Brain-Derived Neurotrophic Factor and the Plasticity of the Mesolimbic Dopamine Pathway.
    Int. Rev. Neurobiol. 2004, 59, 425-444.

  4. T. Mikó, X. Ligneau, H. H. Pertz, J.-M. Arrang, C. R. Ganellin, J.-C. Schwartz, W. Schunack and H. Stark
    Structural Variations of 1-(4-(Phenoxymethyl)benzyl)piperidines as Nonimidazole Histamine H3 Receptor Antagonists.
    Bioorg. Med. Chem. 2004, 12, 2727-2783.

  5. G. Meier, M. Krause, A. Hüls, X. Ligneau, H. H. Pertz, J.-M. Arrang, C. R. Ganellin, J.-C. Schwartz, W. Schunack and H. Stark
    4-(    w-(Alkyloxy)alkyl)-1H-imidazole Derivatives as Histamine H3 Receptor Antagonists / Agonists.
    J. Med. Chem. 2004, 47, 2678-2687.

  6. N. Pelloux-Léon, A. Fkyerat, A. Piripitsi, W. Tertiuk, W. Schunack, H. Stark, M. Garbarg, X. Ligneau, J.-M. Arrang, J.-C. Schwartz and C. R. Ganellin
    Meta-Substituted Aryl(thio)ethers as Potent Partial Agonists (or Antagonists) for the Histamine H3 Receptor Lacking a Nitrogen Atom in the Side Chain.
    J. Med. Chem. 2004, 47, 3264-3274.

  7. M. Schubert-Zsilavecz und H. Stark
    Wiederaufnahme-Hemmung an der Präsynapse als Wirkprinzip:
    Medizinische Chemie moderner Antidepressiva – Targets und Arzneistoffe.
    [Resumption-Inhibition in Presynaptic Action: The Medicinal Chemistry of Modern Antidepressants.]
    Pharm. unsere Zeit 2004, 33, 282-287.

  8. H. Stark, M. Kathmann, E. Schlicker, W. Schunack, B. Schlegel and W. Sippl
    Medicinal Chemical and Pharmacological Aspects of Imidazole-Containing Histamine H3 Receptor Antagonists.
    Mini Rev. Curr. Med.     Chem. 2004, 4, 965-977.

  9. S. Graßmann, J. Apelt, X. Ligneau, H. H. Pertz, J.-M. Arrang, C. R. Ganellin, J.-C. Schwartz, W. Schunack and H. Stark
    Sear    ch for Histamine H3 Receptor Antagonists with Combined Inhibitory Potency at N-Methyltransferase: w-Piperidinoalkanamine Derivatives.
    Arch. Pharm. Pharm. Med. Chem. 2004, 337, 533-545.

  10. A. Lozada, A. A. Aarnisalo, K. Karlstedt, H. Stark and P. Panula
    Plasticity of Histamine H3 Receptor Expression and Binding in the Vestibular Nuclei after Labyrinthectomy in Rat.
    BMC Neuroscience 2004, 5, 32.
    doi:10.1186/1471-2202-5-32; http://www.biomedcentral.com/1471-2202/5/32

  11. B. Sadek, S. Elz, H. H. Pertz, H. Stark and W. Schunack
    Unexpected Partial H1-Receptor Agonism of Imidazole-Type Histamine H3-Receptor Antagonists Lacking a Basic Side-Chain.
    Inflamm. Res. 2004, 53 (Suppl. 2), S109-S115.

  12. P. P. Griffin, M. Schubert-Zsilavecz and H. Stark
    Hemmstoffe von ß-Adrenozeptoren: Gemeinsamkeiten und Unterschiede.
    [Common Properties and Distinctions: Inhibitors of ß-Adrenoceptors.]
    Pharm. unserer Zeit 2004, 33, 442-449.

  13. H. Stark
    Turning from Monogamy to Strategic Promiscuity.
    Drug Discov. Today 2004, 9, 736-737.






    2003

  1. S. Liedtke, K. Flau, M. Kathmann, E. Schlicker, H. Stark, G. Meier and W. Schunack
    Replacement of Imidazole by a Piperidine Moiety Differentially Affects the Potency of Histamine H3-Receptor Antagonists.
    Naunyn-Schmiedeberg´s Arch. Pharmacol. 2003, 367, 43-50.

  2. E. Bézard, S. Ferry, U. Mach, H. Stark, L. Leriche, T. Boraud, C. Gross and P. Sokoloff
    Attenuation of Levodopa-Induced Dyskinesia by Normalizing Dopamine D3 Receptor Function.
    Nat. Med. 2003, 9(6), 762-767.

  3. T. Mikó, X. Ligneau, H. H. Pertz, C. R. Ganellin, J.-M. Arrang, J.-C. Schwartz, W. Schunack and H. Stark
    Novel Nonimidazole Histamine H3 Receptor Antagonists: 1-(4-(Phenoxymethyl)benzyl)­piperidines and Related Compounds.
    J. Med.     Chem. 2003, 46, 1523-1530.

  4. S. Graßmann, J. Apelt, W. Sippl, X. Ligneau, H. H. Pertz, Y. H. Zhao, J.-M. Arrang, C. R. Ganellin, J.-C. Schwartz, W. Schunack and H. Stark
    Imidazole Derivatives as a Novel Class of Hybrid Compounds with Inhibitory Histamine N-Methyltransferase Potencies and Histamine hH3 Receptor Affinities.
    Bioorg.     Med. Chem. 2003, 11(10), 2163-2174.

  5. A. Hackling, R. Ghosh, S. Perachon, A. Mann, H.-D. Höltje, C. G. Wermuth, J.-C. Schwartz, W. Sippl, P. Sokoloff and H. Stark
    N-(w-(4-(2-Methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as Dopamine D2 and D3 Receptor Ligands.
    J. Med. Chem. 2003, 46, 3883-3899.

  6. H. Stark
    Recent Advances in Histamine H3/H4 Receptor Ligands.
    Expert Opin. Ther. Patents 2003, 13(6), 851-865 (Review).

  7. J.-C. Schwartz, S. Morisset, A. Rouleau, X. Ligneau, F. Gbahou, J. Tardivel-Lacombe, H. Stark, W. Schunack, C. R. Ganellin and J.-M. Arrang
    Therapeutic Implications of Constitutive Activity of Receptors: The Example of the Histamine H    3Receptor.
    J. Neural Transm. 2003, 64 Suppl., 1-16.

  8. F. Gbahou, A. Rouleau, S. Morisset, R. Parmentier, S. Crochet, J.-S. Lin, X. Ligneau, J. Tardivel-Lacombe, H. Stark, W. Schunack, C. R. Ganellin, J.-C. Schwartz and J.-M. Arrang
    Protean Agonism at Histamine H3 Receptors in Vitro and in Vivo.
    Proc. Natl.     Acad. Sci. U.S.A. 2003, 100, 11086-11091.

  9. H. Stark
    Wirkmechanismus von HMG-CoA-Reduktase-Inhibitoren – Medizinisch-chemische Aspekte von Statinen.
    [Mechanism of Action of HMG-CoA Reductase Inhibitors. Medical-Chemical Aspects of Statins.]
    Pharm. unserer Zeit 2003, 32 (6), 464-470.





    2002

  1. M. Więcek, K. Kieć-Kononowicz, A. Sasse, X. Ligneau, J.-C. Schwartz, W. Schunack and H. Stark
    Impact of Lipophilicity on the Pharmacological Properties of Histamine H3-Receptor Antagonists of the Cycloalkyl Carbamate Class.
    Inflamm. Res. 2002, 51 (Suppl. 1), S71–S72.

  2. G. Meier, X. Ligneau, H. Pertz, C. R. Ganellin, J.-C. Schwartz, W. Schunack and H. Stark
    Piperidino-Hydrocarbon Compounds as Novel Non-Imidazole Histamine H3-Receptor Antagonists.
    Bioorg. Med. Chem. 2002, 10, 2535–2542.

  3. J. Apelt, X. Ligneau, H. H. Pertz, J.-M. Arrang, C. R. Ganellin, J.-C. Schwartz, W. Schunack and H. Stark
    Development of a New Class of Nonimidazole Histamine H3 Receptor Antagonist with Combined Inhibitory Histamine N-Methyltransferase Activity.
    J. Med. Chem. 2002, 45, 1128–1141.

  4. S. Graßmann, B. Sadek, X. Ligneau, S. Elz, C. R. Ganellin, J.-C. Schwartz, H. Stark and W. Schunack
    Progress in the Proxifan Class: Heterocyclic Congeners as Novel Potent and Selective Histamine H3-Receptor Antagonists.
    Eur. J. Pharm.     Sci. 2002, 15, 367–378.

  5. A. Sasse, X. Ligneau, A. Rouleau, S. Elz, C. R. Ganellin, J.-M. Arrang, J.-C. Schwartz, W. Schunack and H. Stark
    Influence of Bulky Substituents on Histamine H3 Receptor Agonist/Antagonist Properties.
    J. Med.     Chem. 2002, 45, 4000–4010.

  6. D. Łażewska, K. Kieć-Kononowicz, H. H. Pertz, H. Stark and W. Schunack
    Piperidine-Containing Histamine H3-Receptor Antagonists of the Carbamate Series: The Influence of the Additional Ether Functionality.
    Pharmazie 2002, 57(12), 791-795.

  7. A. E. Hackling and H. Stark
    Dopamine D3 Receptor Ligands with Antagonist Properties.
    ChemBioChem 2002, 3, 946-961 (Review).




    2001

  1. H. Stark, M. Krause, A. Rouleau, M. Garbarg, J.-C. Schwartz and W. Schunack
    Enzyme-Catalyzed Prodrug Approaches for the Histamine H3-Receptor Agonist (R)-a-Methylhistamine.
    Bioorg. Med. Chem. 2001, 9, 191-198.

  2. A. Sasse, W. Schunack and H. Stark
    Separation of Chiral 4-Substituted Imidazole Derivatives by Cyclodextrin-Modified Capillary Electrophoresis.
    Biomed. Chromatogr.     2001, 15, 25-30.

  3. A. Sasse, X. Ligneau, B. Sadek, S. Elz, H. H. Pertz, C. R. Ganellin, J.-M. Arrang, J.-C. Schwartz, W. Schunack and H. Stark
    Benzophenone Derivatives and Related Compounds as Potent Histamine H3-Receptor Antagonists and Potential PET/SPECT Ligands.
    Arch. Pharm. Pharm.     Med. Chem. 2001, 334, 45-52.

  4. G. Meier, J. Apelt, U. Reichert, S. Graßmann, X. Ligneau, S. Elz, F. Leurquin, C. R. Ganellin, J.-C. Schwartz, W. Schunack and H. Stark
    Influence of Imidazole Replacement in Different Structural Classes of Histamine H3-Receptor Antagonists.
    Eur. J. Pharm. Sci. 2001, 13, 249-259.

  5. H. Stark, W. Sippl, X. Ligneau, J.-M. Arrang, C. R. Ganellin, J.-C. Schwartz and W. Schunack
    Different Antagonist Binding Properties of Human and Rat Histamine H3 Receptors.
    Bioorg. Med. Chem.     Lett. 2001, 11, 951-954.

  6. T. Nickel, U. Bauer, E. Schlicker, M. Kathmann, M. Göthert, A. Sasse, H. Stark and W. Schunack
    Novel Histamine H3-Receptor Antagonists and Partial Agonists with a Non-Aminergic Structure.
    Br. J. Pharmacol. 2001, 132, 1665-1672.

  7. G. Morini, D. Grandi, A. Sasse, H. Stark and W. Schunack
    Gastroprotective Acitivity of the Novel Histamine H3-Receptor Agonist FUB 407.
    Inflamm. Res. 2001, 50 (Suppl. 2), S116-S117.

  8. M. Krause, H. Stark and W. Schunack
    Azomethine Prodrugs of (R)-a-Methylhistamine, a Highly Potent and Selective Histamine H3-Receptor Agonist.
    Curr. Med.     Chem.2001, 8, 1329-1340 (Review).

  9. B. Weber, E. Schlicker, P. Sokoloff and H. Stark
    Identification of the Dopamine Autoreceptor in the Guinea-Pig Retina as D2 Receptor Using Novel Subtype-Selective Antagonists.
    Br. J. Pharmacol.     2001, 133, 1243-1248.

  10. J.-C. Schwartz, S. Morisset, A. Rouleau, J. Tardivel-Lacombe, F. Gbahou, X. Ligneau, A. Heron, A. Sasse, H. Stark, W. Schunack, C. R. Ganellin and J.-M. Arrang
    Application of Genomics to Drug Design: The Example of the Histamine H3 Receptor.
    Eur. Neuropsychopharmacol. 2001, 11, 441-448.

  11. D. Lazewska, K. Kieć-Kononowicz, H. H. Pertz, H. Stark, W. Schunack and S. Elz
    Piperidine-Containing Histamine H3-Receptor Antagonists of the Carbamate Series: Variation of the Spacer Length.
    Pharmazie 2001, 56, 927-932    .






    2000

  1. S. Reidemeister, H. Stark, X. Ligneau, C. R. Ganellin, J.-C. Schwartz and W. Schunack
    Substituted N-Phenyl Carbamates as Histamine H3 Receptor Antagonists with Improved in Vivo Potency.
    Pharmazie 2000, 55, 83-86.

  2. K. Kieć-Kononowicz, M. Więcek, A. Sasse, X. Ligneau, S. Elz, C. R. Ganellin, J.-C. Schwartz, H. Stark and W. Schunack
    Importance of the Lipophilic Group in Carbamates Having Histamine H3-Receptor Antagonist Activity.
    Pharmazie 2000, 55, 349-355.

  3. G. Morini, D. Grandi, H. Stark and W. Schunack
    Histamine H3-Receptor Antagonists Inhibit Gastroprotection by (R)-a-Methylhistamine in the Rat.
    Br. J. Pharmacol. 2000, 129, 1597-1600.

  4. A. Sasse, H. Stark, X. Ligneau, S. Elz, S. Reidemeister, C. R. Ganellin, J.-C. Schwartz and W. Schunack
    (Partial) Agonist/Antagonist Properties of Novel Diarylalkyl Carbamates on Histamine H3 Receptors.
    Bioorg. Med. Chem. 2000, 8, 1139-1149.

  5. H. Stark, S. Graßmann und U. Reichert
    Struktur, Funktion und potentielle therapeutische Bedeutung von NMDA-Rezeptoren.
    Teil 1: Architektur und Modulation der Rezeptoren.
    [Structure, Function and Potential Therapeutic Possibilites of NMDA Receptors.
    1. Architecture and Modulation of Receptors.]
    Pharm. unserer Zeit 2000, 29, 159-166 (Review).

  6. H. Stark, U. Reichert und S. Graßmann
    Struktur, Funktion und potentielle therapeutische Bedeutung von NMDA-Rezeptoren.
    Teil 2: Therapiekonzepte und neue Rezeptorliganden.
    [Structure, Function and Potential Therapeutic Possibilities of NMDA Receptors.
    2. Therapy Concepts and New Receptor Ligands.]
    Pharm. unserer Zeit 2000, 29, 228-236 (Review).

  7. A. Sasse, B. Sadek, X. Ligneau, S. Elz, H. H. Pertz, P. Luger, C. R. Ganellin, J.-M. Arrang, J.-C. Schwartz, W. Schunack and H. Stark
    New Histamine H3-Receptor Ligands of the Proxifan Series: Imoproxifan and Other Selective Antagonists with High Oral in Vivo Potency.
    J. Med. Chem. 2000, 43, 3335-3343.

  8. A. Rouleau, H. Stark, W. Schunack and J.-C. Schwartz
    Anti-Inflammatory and Antinociceptive Properties of BP 2-94, a Histamine H3-Receptor Agonist Prodrug.
    J. Pharmacol. Exp. Ther. 2000, 295, 219-225.

  9. H. Stark, X. Ligneau, B. Sadek, C. R. Ganellin, J.-M. Arrang, J.-C. Schwartz and W. Schunack
    Analogues and Derivatives of Ciproxifan, a Novel Prototype for Generating Potent Histamine H3-Receptor Antagonists.
    Bioorg. Med. Chem.     Lett.2000, 10, 2379-2382.

  10. H. Stark, B. Sadek, M. Krause, A. Hüls, X. Ligneau, C. R. Ganellin, J.-M. Arrang, J.-C. Schwartz and W. Schunack
    Novel Histamine H3-Receptor Antagonists with Carbonyl-Substituted 4-(3-(Phenoxy)propyl)-1H-imidazole Structures like Ciproxifan and Related Compounds.
    J. Med.     Chem. 2000, 43, 3987-3994.

  11. S. Morisset, A. Rouleau, X. Ligneau, F. Gbahou, J. Tardivel-Lacombe, H. Stark, W. Schunack, C. R. Ganellin, J.-C. Schwartz and J.-M. Arrang
    High Constitutive Activity of Native H3 Receptor Regulates Histamine Neurones in Brain.
    Nature (London) 2000, 408, 860-864.

  12. X. Ligneau, S. Morisset, J. Tardivel-Lacombe, F. Gbahou, C. R. Ganellin, H. Stark, W. Schunack, J.-C. Schwartz and J.-M. Arrang
    Distinct Pharmacology of Rat and Human Histamine H3 Receptors: Role of Two Amino Acids in the Third Transmembrane Domain.
    Br. J. Pharmacol. 2000, 131, 1247-1250 (Special Report).

  13. H. Stark
    Convenient Procedures for Synthesis of Ciproxifan, a Histamine H3-Receptor Antagonist.
    Arch. Pharm. Pharm.     Med. Chem. 2000, 333, 315-316.




    1999

  1. A. Sasse, K. Kieć-Kononowicz, H. Stark, M. Motyl, S. Reidemeister, C. R. Ganellin, X. Ligneau, J.-C. Schwartz and W. Schunack
    Development of Chiral N-Alkyl Carbamates as New Leads for Potent and Selective H3-Receptor Antagonists: Synthesis, Capillary Electrophoresis, and in Vitro and Oral in Vivo Activity.
    J. Med. Chem. 1999, 42, 593-600.

  2. N. Matzanke, W. Löwe, S. Perachon, P. Sokoloff, J.-C. Schwartz and H. Stark
    Heterocyclic Congeners of PD 128,907 with a Partially Hydrogenated Benzomorpholine Moiety as Potential Dopamine D3-Receptor Ligands.
    Eur. J. Med. Chem. 1999, 34, 791-798.

  3. A. D. Windhorst, H. Timmerman, R. P. Klok, F. G. J. Custers, W. M. P. B. Menge, R. Leurs, H. Stark, W. Schunack, E. G. J. Gielen, M. J. P. G.    van Kroonen­burgh and J. D. M. Herscheid
    Radiosynthesis and Biodistribution of 123I-Labeled Antagonists of the Histamine H3 Receptor as Potential SPECT Ligands.
    Nucl. Med. Biol. 1999, 26, 651-659.

  4. A. Sasse, H. Stark, S. Reidemeister, A. Hüls, S. Elz, X. Ligneau, C. R. Ganellin, J.-C. Schwartz and W. Schunack
    Novel Partial Agonists for the Histamine H3 Receptor with High in Vitro and in Vivo Activity.
    J. Med. Chem. 1999, 42, 4269-4274.

  5. A. D. Windhorst, H. Timmerman, R. P. Klok, F. G. J. Custers, W. M. P. B. Menge, R. Leurs, H. Stark, W. Schunack, M. J. P. G. van Kroonenburgh and J. D. M. Herscheid
    Radiosynthesis and Biodistribution of 123I Labeled Antagonists as Potential SPECT Ligands for the Histamine H3 Receptor.
    J. Labell. Compd. Radiopharm. 1999, 42 (Suppl. 1), S282-S284.





    1998

  1. H. Stark, A. Hüls, X. Ligneau, K. Purand, H. Pertz, J.-M. Arrang, J.-C. Schwartz and W. Schunack
    Development of FUB 181, a Selective Histamine H3-Receptor Antagonist of High Oral in Vivo Potency with         4-(w-(Arylalkyloxy)alkyl)-1H-imidazole Structure.
    Arch. Pharm. Pharm. Med. Chem. 1998, 331, 211-218.

  2. K. Onodera, S. Miyazaki, M. Imaizumi, H. Stark and W. Schunack
    Improvement by FUB 181, a Novel Histamine H3-Receptor Antagonist, of Learning and Memory in the Elevated Plus-Maze Test in Mice.
    Naunyn-Schmiedeberg´s Arch. Pharmacol. 1998, 357, 508-513.

  3. W. Sippl, H. Stark and H.-D. Höltje
    Development of a Binding Site Model for Histamine H    3-Receptor Agonists.
    Pharmazie 1998, 53, 433-437.

  4. X. Ligneau, J.-S. Lin, G. Vanni-Mercier, M. Jouvet, J. L. Muir, C. R. Ganellin, H. Stark, S. Elz, W. Schunack and J.-C. Schwartz
    Neurochemical and Behavioral Effects of Ciproxifan, a Potent Histamine H3-Receptor Antagonist.      
    J. Pharmacol. Exp. Ther. 1998, 287, 658-666.

  5. A. Lecklin, P. Etu-Seppälä, H. Stark and L. Tuomisto
    Effects of Intracerebroventricular Infused Histamine and Selective H1, H2 and H3 Agonists on Food and Water Intake and Urine Flow in Wistar Rats.
    Brain Res. 1998, 793, 279-288.

  6. H. Stark, X. Ligneau, J.-M. Arrang, J.-C. Schwartz and W. Schunack
    General Construction Pattern of Histamine H3-Receptor Antagonists: Change of a Paradigm.
    Bioorg. Med. Chem.     Lett. 1998, 8, 2011-2016.

  7. M. Krause, X. Ligneau, H. Stark, M. Garbarg, J.-C. Schwartz and W. Schunack
    4-Alkynylphenyl Imidazolpropyl Ethers as Selective Histamine H3-Receptor Antagonists with High Oral Central Nervous System Activity.
    J. Med. Chem. 1998, 41, 4171-4176.

  8. M. Kathmann, E. Schlicker, I. Marr, S. Werthwein, H. Stark and W. Schunack
    Ciproxifan and Chemically Related Compounds are Highly Potent and Selective Histamine H3-Receptor Antagonists.
    Naunyn-Schmiedeberg´s Arch. Pharmacol. 1998, 358, 623-627.






    1997

  1. H. Stark, X. Ligneau, R. Lipp, J.-M. Arrang, M. Garbarg, J.-C. Schwartz and W. Schunack
    Search for Novel Leads for Histamine H3-Receptor Antagonists: Amine Derivatives.
    Pharmazie 1997, 52, 419-423.

  2. A. Rouleau, M. Garbarg, X. Ligneau, C. Mantion, P. Lavie, C. Advenier, J.-M. Lecomte, M. Krause, H. Stark, W. Schunack and J.-C. Schwartz
    Bioavailability, Antinociceptive and Antiinflammatory Properties of BP 2-94, an Histamine H3 Receptor Agonist Prodrug.
    J. Pharmacol. Exp. Ther. 1997, 281, 1085-1094.

  3. H. Stark, A. Hüls, X. Ligneau, J.-M. Arrang, J.-C. Schwartz and W. Schunack
    Search for Novel Leads for Histamine H3-Receptor Antagonists: Oxygen-containing Derivatives,
    Pharmazie 1997, 52, 495-500.

  4. S. Corbel, E. Traiffort, H. Stark, W. Schunack and M. Dy
    Binding of Histamine H3-Receptor Antagonists to Hematopoietic Progenitor Cells: Evidence for a Histamine Transporter Unrelated to Histamine H3 Receptors.
    FEBS Lett. 1997, 404, 289-293.

  5. M. Krause, H. Stark and W. Schunack
    Iododestannylation: An Improved Synthesis of [125I]Iodoproxyfan, a Specific Radioligand of the Histamine H3-Receptor.
    J. Labell. Compd. Radiopharm. 1997, 39, 601-606.






    1996

  1. H. Stark, K. Purand, X. Ligneau, A. Rouleau, J.-M. Arrang, M. Garbarg, J.-C. Schwartz and W. Schunack
    Novel Carbamates as Potent Histamine H3 Receptor Antagonists with High in Vitro and Oral in Vivo Activity.
    J. Med. Chem. 1996, 39, 1157-1163.

  2. H. Stark, K. Purand, A. Hüls, X. Ligneau, M. Garbarg, J.-C. Schwartz and W. Schunack
    [125I]Iodoproxyfan and Related Compounds: A Reversible Radioligand and Novel Classes of Antagonists with High Affinity and Selectivity for the Histamine H3 Receptor.
    J. Med. Chem. 1996, 39, 1220-1226.

  3. E. Schlicker, M. Kathmann, H. Bitschnau, I. Marr, S. Reidemeister, H. Stark and W. Schunack
    Potencies of Antagonists Chemically Related to Iodoproxyfan at Histamine H3 Receptors in Mouse Brain Cortex and Guinea-pig Ileum: Evidence for H3 Receptor Heterogeneity?
    Naunyn-Schmiedeberg´s Arch. Pharmacol. 1996, 353, 482-488.

  4. M. Krause, A. Rouleau, H. Stark, P. Luger, M. Garbarg, J.-C. Schwartz and W. Schunack
    New Potent Azomethine Prodrugs of the Histamine H3-Receptor Agonist (R)-a-Methylhistamine Containing a Heteroarylphenyl Partial Structure.
    Arch. Pharm. Pharm.     Med. Chem. 1996, 329, 209-215.

  5. H. Stark, E. Schlicker and W. Schunack
    Developments of Histamine H3-Receptor Antagonists.
    Drugs Future 1996, 21, 507-520 (Review).

  6. A. Hüls, K. Purand, H. Stark, S. Reidemeister, X. Ligneau, M. Garbarg, J.-C. Schwartz and W. Schunack
    Novel Histamine H3-Receptor Antagonists with Benzyl Structure or Related Moieties: Synthesis and Structure-Activity Relationships.
    Arch. Pharm. Pharm. Med. Chem. 1996, 329, 379-385.

  7. A. Hüls, K. Purand, H. Stark, X. Ligneau, J.-M. Arrang, J.-C. Schwartz and W. Schunack
    Diphenylmethy Ethers: Synthesis and Histamine H3-Receptor Antagonist in Vitro and in Vivo Activity.
    Bioorg. Med. Chem.     Lett. 1996, 6, 2013-2018.

  8. M. Krause, A. Rouleau, H. Stark, M. Garbarg, J.-C. Schwartz and W. Schunack
    Structure-Activity Relationships of Novel Azomethine Prodrugs of the Histamine H3-Receptor Agonist (R)-a-Methylhistamine: From Alkylaryl to Substituted Diaryl Derivatives.
    Pharmazie 1996, 51, 720-726.

  9. M. Krause, A. Rouleau, H. Stark, M. Garbarg, J.-C. Schwartz and W. Schunack
    Relationship between Lipophilicity and Brain Uptake of Azomethine Prodrugs of a Histamine H3-Receptor Agonist.
    Sci. Pharm. 1996, 64, 503-509.






    1995

  1. R. Lipp, H. Stark, J. M. Arrang, M. Garbarg, J. C. Schwartz and W. Schunack
    Synthesis and Histamine H3-Receptor Agonist Activity of Mono- and Dialkyl-Substituted Histamine Derivatives.
    Eur. J. Med. Chem. 1995, 30, 219-225.

  2. H. Stark, R. Lipp, J.-M. Arrang, M. Garbarg, X. Ligneau, J.-C. Schwartz and W. Schunack
    New Potent Histamine H3-Receptor Antagonists of the Amide Type
    Eur. J. Pharm. Sci. 1995, 3, 95-104.

  3. W. Sippl, H. Stark and H. D. Höltje
    Computer-Assisted Analysis of Histamine H2- and H3-Receptor Agonists.
    Quant. Struct.-Act.     Relation. 1995, 14, 121-125.

  4. K. Kieć-Kononowicz, X. Ligneau, H. Stark, J.-C. Schwartz and W. Schunack
    Azines and Diazines as Potential Histamine H3-Receptor Antagonists.
    Arch. Pharm. (Weinheim) 1995, 328, 445-450.

  5. M. Krause, A. Rouleau, H. Stark, P. Luger, R. Lipp, M. Garbarg, J.-C. Schwartz and W. Schunack
    Synthesis, X-ray Crystallography, and Pharmacokinetics of Novel Azomethine Prodrugs of (R)-a-Methylhistamine: Highly Potent and Selective Histamine H3 Receptor Agonists.
    J. Med. Chem. 1995, 38, 4070-4079.






    1994

  1. E. Schlicker, M. Kathmann, S. Reidemeister, H. Stark and W. Schunack
    Novel Histamine H3 Receptor Antagonists: Affinities in an H3 Receptor Binding Assay and Potencies in Two Functional H3 Receptor Models.
    Br. J. Pharmacol. 1994, 112, 1043-1048; ibid. 1994, 113, 637.

  2. H. Stark, R. Lipp, J.-M. Arrang, M. Garbarg, J.-C. Schwartz and W. Schunack
    Acylated and Alkylated Histamine Derivatives as New Histamine H3-Receptor Antagonists.
    Eur. J. Med. Chem. 1994, 29, 695-700.

  3. W. Schunack and H. Stark
    Design of Histamine H3-Receptor Agonists and Antagonists.
    Eur. J. Drug Metab. Pharmacokin. 1994, 19, 173-178 (Review).

  4. X. Ligneau, M. Garbarg, M. L. Vizuete, J. Diaz, K. Purand, H. Stark, W. Schunack and J.-C. Schwartz
    [125I]Iodoproxyfan, a New Antagonist to Label and Visualize Cerebral Histamine H3 Receptors.
    J. Pharmacol. Exp. Ther. 1994, 271, 452-459.

  5. H. Stark, M. Krause, J.-M. Arrang, X. Ligneau, J.-C. Schwartz and W. Schunack
    Unsymmetrically Substituted Guanidines as Potent Histamine H3-Receptor Antagonists.
    Bioorg. Med. Chem.     Lett. 1994, 4, 2907-2912.






    1991

  1. E. Poli, H. Stark and G. Bertaccini
    Histami    ne H3-Receptor Activation Inhibits Acetylcholine Release from the Guinea Pig Myenteric Plexus.
    Agents Actions 1991, 33, 167-169.

  2. H. Stark
    Zur Arzneistoffentwicklung von Prodrugs mit agonistischer Wirkform und Antagonisten des Histamin-H3-Rezeptors.
    Dissertation, Freie Universität Berlin, Berlin, Germany, 1991.

 

 

 

 

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