C E Muller

Summary

Affiliation: University of Bonn
Country: Germany

Publications

  1. ncbi request reprint 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors
    Vita Ozola
    University of Bonn, Pharmaceutical Institute Poppelsdorf, Kreuzbergweg 26, D 53115 Bonn, Germany
    Bioorg Med Chem 11:347-56. 2003
  2. doi request reprint Allosteric modulators of rhodopsin-like G protein-coupled receptors: opportunities in drug development
    Christa E Muller
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D 53121 Bonn, Germany
    Pharmacol Ther 135:292-315. 2012
  3. doi request reprint Convergent synthesis of the potent P2Y receptor antagonist MG 50-3-1 based on a regioselective Ullmann coupling reaction
    Younis Baqi
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, Pharmaceutical Sciences Bonn PSB, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    Molecules 17:2599-615. 2012
  4. pmc [(3)H]Adenine is a suitable radioligand for the labeling of G protein-coupled adenine receptors but shows high affinity to bacterial contaminations in buffer solutions
    Anke C Schiedel
    University of Bonn, Pharmaceutical Institute, Pharmaceutical Sciences Bonn PSB, Pharmaceutical Chemistry I, Bonn, Germany
    Purinergic Signal 3:347-58. 2007
  5. pmc Structure-activity relationships of anthraquinone derivatives derived from bromaminic acid as inhibitors of ectonucleoside triphosphate diphosphohydrolases (E-NTPDases)
    Younis Baqi
    Pharmaceutical Institute, Pharmaceutical Sciences Bonn PSB, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121, Bonn, Germany
    Purinergic Signal 5:91-106. 2009
  6. ncbi request reprint Interactions of valerian extracts and a fixed valerian-hop extract combination with adenosine receptors
    Christa E Muller
    Universitat Bonn, Pharmazeutisches Institut, Pharmazeutische Chemie Poppelsdorf, Kreuzbergweg 26, D 53115 Bonn, Germany
    Life Sci 71:1939-49. 2002
  7. ncbi request reprint Polyoxometalates--a new class of potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitors
    Christa E Muller
    Pharmaceutical Institute, Pharmaceutical Sciences Bonn PSB, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    Bioorg Med Chem Lett 16:5943-7. 2006
  8. ncbi request reprint Medicinal chemistry of adenosine A3 receptor ligands
    Christa E Muller
    Pharmaceutical Institute, University of Bonn, Germany
    Curr Top Med Chem 3:445-62. 2003
  9. ncbi request reprint Xanthines as adenosine receptor antagonists
    Christa E Muller
    University of Bonn, Pharmaceutical Institute, An der Immenburg 4, 53121, Bonn, Germany
    Handb Exp Pharmacol 200:151-99. 2011
  10. ncbi request reprint A(3) adenosine receptor antagonists
    C E Muller
    Pharmaceutical Institute, University of Bonn, Germany
    Mini Rev Med Chem 1:417-27. 2001

Collaborators

Detail Information

Publications67

  1. ncbi request reprint 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors
    Vita Ozola
    University of Bonn, Pharmaceutical Institute Poppelsdorf, Kreuzbergweg 26, D 53115 Bonn, Germany
    Bioorg Med Chem 11:347-56. 2003
    ..Due to their high A(3) affinity, selectivity, and relatively high water-solubility, 2-phenyl-imidazo[2,1-i]purin-5-ones may become useful research tools...
  2. doi request reprint Allosteric modulators of rhodopsin-like G protein-coupled receptors: opportunities in drug development
    Christa E Muller
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D 53121 Bonn, Germany
    Pharmacol Ther 135:292-315. 2012
    ..The development of allosteric modulators for rhodopsin-like GPCRs as novel drugs is still at an early stage; it appears highly promising...
  3. doi request reprint Convergent synthesis of the potent P2Y receptor antagonist MG 50-3-1 based on a regioselective Ullmann coupling reaction
    Younis Baqi
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, Pharmaceutical Sciences Bonn PSB, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    Molecules 17:2599-615. 2012
    ..A new synthon (sodium 2-(4,6-dichloro-1,3,5-triazin-2-ylamino)benzenesulfonate, 13) which can easily be obtained on a gram scale was prepared, and 13 was successfully coupled with 8 yielding the target compound 3...
  4. pmc [(3)H]Adenine is a suitable radioligand for the labeling of G protein-coupled adenine receptors but shows high affinity to bacterial contaminations in buffer solutions
    Anke C Schiedel
    University of Bonn, Pharmaceutical Institute, Pharmaceutical Sciences Bonn PSB, Pharmaceutical Chemistry I, Bonn, Germany
    Purinergic Signal 3:347-58. 2007
    ..We conclude that [(3)H]adenine is a well-suitable radioligand for adenine receptor binding studies but that bacterial contamination of the employed buffer solutions must be avoided...
  5. pmc Structure-activity relationships of anthraquinone derivatives derived from bromaminic acid as inhibitors of ectonucleoside triphosphate diphosphohydrolases (E-NTPDases)
    Younis Baqi
    Pharmaceutical Institute, Pharmaceutical Sciences Bonn PSB, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121, Bonn, Germany
    Purinergic Signal 5:91-106. 2009
    ..328 muM) and NTPDase3 (K(i) 2.22 muM). Its isomer, 1-amino-2-sulfo-4-(1-naphthylamino)anthraquinone (20), was a potent and selective inhibitor of rat NTPDase3 (K(i) 1.5 muM)...
  6. ncbi request reprint Interactions of valerian extracts and a fixed valerian-hop extract combination with adenosine receptors
    Christa E Muller
    Universitat Bonn, Pharmazeutisches Institut, Pharmazeutische Chemie Poppelsdorf, Kreuzbergweg 26, D 53115 Bonn, Germany
    Life Sci 71:1939-49. 2002
    ..In addition valerian extract inhibited cAMP accumulation in CHO-hA(1) cell membranes. The partial agonistic activity at A(1)ARs may thus play a role in the sleep inducing effect of Ze 91019 and the valerian extract therein...
  7. ncbi request reprint Polyoxometalates--a new class of potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitors
    Christa E Muller
    Pharmaceutical Institute, Pharmaceutical Sciences Bonn PSB, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    Bioorg Med Chem Lett 16:5943-7. 2006
    ..One of the compounds, (NH(4))(18)[NaSb(9)W(21)O(86)], was selective for NTPDases2 and 3 versus NTPDase1. NTPDase inhibition might contribute to the described biological effects of polyoxometalates, including their anti-cancer activity...
  8. ncbi request reprint Medicinal chemistry of adenosine A3 receptor ligands
    Christa E Muller
    Pharmaceutical Institute, University of Bonn, Germany
    Curr Top Med Chem 3:445-62. 2003
    ....
  9. ncbi request reprint Xanthines as adenosine receptor antagonists
    Christa E Muller
    University of Bonn, Pharmaceutical Institute, An der Immenburg 4, 53121, Bonn, Germany
    Handb Exp Pharmacol 200:151-99. 2011
    ..A large number of derivatives and analogues were subsequently synthesized and evaluated as AR antagonists. Very potent antagonists have thus been developed with selectivity for each of the four AR subtypes...
  10. ncbi request reprint A(3) adenosine receptor antagonists
    C E Muller
    Pharmaceutical Institute, University of Bonn, Germany
    Mini Rev Med Chem 1:417-27. 2001
    ..Most of the A(3) AR antagonists are highly lipophilic and exhibit very poor water-solubility. Potential therapeutic applications for A(3) AR antagonists include inflammatory diseases, asthma, stroke, and glaucoma...
  11. ncbi request reprint P2-pyrimidinergic receptors and their ligands
    Christa E Muller
    Pharmaceutical Institute, University of Bonn, Germany
    Curr Pharm Des 8:2353-69. 2002
    ..P2Y(2) agonists are currently in clinical development for cystic fibrosis and dry eye syndrome. Selective antagonists for pyrimidinergic P2Y receptors are still lacking...
  12. doi request reprint Prodrug approaches for enhancing the bioavailability of drugs with low solubility
    Christa E Muller
    PharmaCenter Bonn, University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D 53121 Bonn
    Chem Biodivers 6:2071-83. 2009
    ..Prodrug approaches will already be considered in the early phase of drug discovery...
  13. ncbi request reprint Adenosine receptor ligands-recent developments part I. Agonists
    C E Muller
    Pharmaceutical Institute, University of Bonn, Bonn, Germany
    Curr Med Chem 7:1269-88. 2000
    ....
  14. ncbi request reprint A1 adenosine receptors and their ligands: overview and recent developments
    C E Muller
    University of Bonn, Pharmaceutical Institute, Department of Pharmaceutical Chemistry, Germany
    Farmaco 56:77-80. 2001
    ..18F- and 11C-labeled A1 AR antagonists have been developed for positron emission tomography studies...
  15. ncbi request reprint [(3)H]8-Ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one ([(3)H]PSB-11), a novel high-affinity antagonist radioligand for human A(3) adenosine receptors
    Christa E Muller
    Pharmaceutical Institute, University of Bonn, Kreuzbergweg 26, D 53115 Bonn, Germany
    Bioorg Med Chem Lett 12:501-3. 2002
    ..The new radioligand shows an extraordinarily low degree of non-specific binding rendering it a very useful tool for studying the (patho)physiological roles of A(3 )ARs...
  16. pmc Recent developments in adenosine receptor ligands and their potential as novel drugs
    Christa E Muller
    University of Bonn, An der Immenburg 4, Bonn, Germany
    Biochim Biophys Acta 1808:1290-308. 2011
    ....
  17. ncbi request reprint Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists
    Christa E Muller
    Pharmaceutical Institute Poppelsdorf, University of Bonn, Bonn, Germany
    J Med Chem 45:3440-50. 2002
    ..The most potent A(3) antagonist of the present series was (R)-4-methyl-8-ethyl-2-phenyl-imidazo[2,1-i]purin-5-one (R-24) exhibiting a K(i) value of 2.3 nM and high selectivity for A(3) receptors vs all other AR subtypes...
  18. ncbi request reprint Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability
    Luo Yan
    University of Bonn, Pharmaceutical Chemistry Poppelsdorf, Pharmaceutical Sciences, Bonn, Germany
    J Med Chem 47:1031-43. 2004
    ..This new protection strategy allowed for the upscaling of the synthesis of 1-propyl-8-p-sulfophenylxanthine (PSB-1115), a selective A(2B) antagonist...
  19. ncbi request reprint Development of spin-labeled probes for adenosine receptors
    Janez Ilas
    Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Kreuzbergweg 26, D 53113 Bonn, Germany
    J Med Chem 48:2108-14. 2005
    ..The novel spin-labeled A(1)-selective or A(1)/A(2B)-nonselective adenosine receptor antagonists may become useful probes for biophysicochemical investigations of adenosine receptors in their membrane environment...
  20. ncbi request reprint Adenosine receptor agonists: from basic medicinal chemistry to clinical development
    Luo Yan
    University of Bonn, Pharmaceutical Institute Poppelsdorf, Kreuzbergweg 26, D 53115 Bonn, Germany
    Expert Opin Emerg Drugs 8:537-76. 2003
    ..Partial agonists, inhibitors of adenosine metabolism (adenosine kinase and deaminase inhibitors) or allosteric activators of adenosine receptors may be advantageous for certain indications, as they may exhibit fewer side effects...
  21. doi request reprint High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors
    Younis Baqi
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, Pharmaceutical Sciences Bonn, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    J Med Chem 52:3784-93. 2009
    ..Compounds 39 and 41 represent new lead structures for the development of antithrombotic drugs...
  22. ncbi request reprint Tricyclic theophylline derivatives with high water-solubility: structure-activity relationships at adenosine receptors, phosphodiesterases, and benzodiazepine binding sites
    U Geis
    Pharmazeutisches Institut, Universitat Tubingen, Germany
    Pharmazie 50:333-6. 1995
    ..Two compounds were found to show an about 10-fold affinity for benzodiazepine binding sites compared with caffeine and theophylline...
  23. ncbi request reprint 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists
    Alaa M Hayallah
    University of Bonn, Pharmaceutical Institute Poppelsdorf, Bonn, Germany
    J Med Chem 45:1500-10. 2002
    ..30-fold selectivity versus rat A1, and greater than 400-fold selectivity versus human A2A and A3 ARs. The new potent, selective, water-soluble A2B antagonists may be useful research tools for investigating A2B receptor function...
  24. ncbi request reprint Interaction of valerian extracts of different polarity with adenosine receptors: identification of isovaltrate as an inverse agonist at A1 receptors
    Svenja K Lacher
    Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, Bonn, Germany
    Biochem Pharmacol 73:248-58. 2007
    ..The common use of hydrophilic, but not lipophilic valerian extracts as mild sleep-inducing agents is consistent with the opposite actions of hydrophilic and lipophilic extracts on adenosine receptors...
  25. ncbi request reprint Cloning and functional expression of a novel Gi protein-coupled receptor for adenine from mouse brain
    Ivar von Kügelgen
    Department of Pharmacology and Toxicology, University of Bonn, D 53113 Bonn, Germany
    Mol Pharmacol 73:469-77. 2008
    ..In summary, our data show that a second mammalian DNA sequence encodes for a G(i)-coupled GPCR activated by low, nanomolar concentrations of adenine...
  26. ncbi request reprint Rapid and efficient microwave-assisted copper(0)-catalyzed ullmann coupling reaction: general access to anilinoanthraquinone derivatives
    Younis Baqi
    Pharmaceutical Institute, University of Bonn, D 53121 Bonn, Germany
    Org Lett 9:1271-4. 2007
    ..The new procedure provides the first general access to anilinoanthraquinones, furnishing a number of previously inaccessible compounds. It is superior to classical methods in all aspects, including yields, reaction time, and versatility...
  27. doi request reprint 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity
    Thomas Borrmann
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, D 53121 Bonn, Germany
    J Med Chem 52:3994-4006. 2009
    ..It was shown to be a useful pharmacological tool for the selective labeling of human as well as rodent A(2B) receptors (K(D) human A(2B) 0.403 nM, mouse A(2B) 0.351 nM)...
  28. doi request reprint Interaction of new, very potent non-nucleotide antagonists with Arg256 of the human platelet P2Y12 receptor
    Kristina Hoffmann
    Department of Pharmacology and Toxicology, University of Bonn, Bonn, Germany
    J Pharmacol Exp Ther 331:648-55. 2009
    ..The results also indicate that the sulfonic acid residue at ring D is involved in the interaction of antagonists derived from reactive blue 2 with the residue Arg256 of the human P2Y(12) receptor...
  29. doi request reprint Structure-activity relationships of adenine and deazaadenine derivatives as ligands for adenine receptors, a new purinergic receptor family
    Thomas Borrmann
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, Bonn, Germany
    J Med Chem 52:5974-89. 2009
    ..0341 microM) were much more potent at the human as compared to the rat binding site. The new AdeR ligands may serve as lead structures and contribute to the elucidation of the functions of the adenine receptor family...
  30. ncbi request reprint Evidence for the functional expression and pharmacological characterization of adenine receptors in native cells and tissues
    Simone Gorzalka
    Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Bonn, Germany
    Mol Pharmacol 67:955-64. 2005
    ..Moreover, preliminary radioligand binding studies with [3H]adenine at membranes of human astrocytoma 1321N1 cells suggest that a human ortholog of the rat adenine receptor exists...
  31. ncbi request reprint Recent progress in the development of adenosine receptor ligands as antiinflammatory drugs
    Rhalid Akkari
    Pharmaceutical Sciences Bonn, PSB, Pharmaceutical Institute, University of Bonn, Germany
    Curr Top Med Chem 6:1375-99. 2006
    ..This review article will focus on compounds published or patented within the past three years...
  32. doi request reprint Synthesis of alkyl- and aryl-amino-substituted anthraquinone derivatives by microwave-assisted copper(0)-catalyzed Ullmann coupling reactions
    Younis Baqi
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, Pharmaceutical Sciences Bonn PSB, University of Bonn, Bonn, Germany
    Nat Protoc 5:945-53. 2010
    ..The reaction is performed without the use of a glove box and there is no requirement for an inert atmosphere. The reaction typically proceeds within 2-30 min, the protocol, including workup, generally takes 1-3 h to complete...
  33. ncbi request reprint A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists
    Luo Yan
    Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Kreuzbergweg 26, D 53115 Bonn, Germany
    J Med Chem 49:4384-91. 2006
    ..6 nM for the human A(2B) receptor combined with high selectivity versus the other human adenosine receptor subtypes (575-fold versus A(1), 134-fold versus A(2A), and >278-fold versus A(3))...
  34. doi request reprint Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold
    Younis Baqi
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, Pharmaceutical Sciences Bonn, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    J Med Chem 53:2076-86. 2010
    ..Investigations of ecto-nucleoside triphosphate diphosphohydrolases (NTPDases) and the P2Y receptor subtypes P2Y(2), P2Y(4), P2Y(6), and P2Y(12) showed that compound 45 exhibited the highest degree of selectivity (>150-fold)...
  35. doi request reprint Adenosine receptor subtype-selective antagonists in inflammation and hyperalgesia
    Andras Bilkei-Gorzo
    Institute of Molecular Psychiatry, University of Bonn, Sigmund Freud Str 25, 53127 Bonn, Germany
    Naunyn Schmiedebergs Arch Pharmacol 377:65-76. 2008
    ..Selective A(2A) antagonists may be useful for the treatment of inflammatory hyperalgesia, while A(2B) antagonists have potential as analgesic drugs for the treatment of inflammatory pain...
  36. doi request reprint Selective nucleoside triphosphate diphosphohydrolase-2 (NTPDase2) inhibitors: nucleotide mimetics derived from uridine-5'-carboxamide
    Andreas Brunschweiger
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, Pharmaceutical Sciences Bonn, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    J Med Chem 51:4518-28. 2008
    ..NTPDase2 inhibitors have potential as novel cardioprotective drugs for the treatment of stroke and for cancer therapy...
  37. ncbi request reprint Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists
    Stefanie Weyler
    Pharmaceutical Institute, Pharmaceutical Sciences Bonn, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    Bioorg Med Chem Lett 18:223-7. 2008
    ..4-Phenylamino-substituted 1-amino-2-sulfoanthraquinones, for example, 1-amino-4-(2-methoxyphenyl)-2-sulfoanthraquinone (PSB-716), were potent P2Y2 antagonists with IC50 values in the low micromolar range...
  38. ncbi request reprint Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A(1) adenosine receptors
    Britta Schumacher
    Pharmaceutical Institute Poppelsdorf, University of Bonn, Germany
    J Nat Prod 65:1479-85. 2002
    ..Lignan 4 is the first nonnucleoside adenosine receptor agonist not structurally related to adenosine...
  39. ncbi request reprint Synthesis and properties of a new water-soluble prodrug of the adenosine A 2A receptor antagonist MSX-2
    Karl Vollmann
    Pharma Center Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D 53121 Bonn, Germany
    Molecules 13:348-59. 2008
    ..It was found to be stable in artificial gastric acid, but readily cleaved by pig liver esterase...
  40. doi request reprint 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists
    Anja B Scheiff
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, D 53121 Bonn, Germany
    Bioorg Med Chem 18:2195-203. 2010
    ..Compound 16 m may serve as a new lead structure for the development of second-generation non-xanthine-derived A(1) antagonists which have potential as novel drugs...
  41. ncbi request reprint Multigram-scale syntheses, stability, and photoreactions of A2A adenosine receptor antagonists with 8-styrylxanthine structure: potential drugs for Parkinson's disease
    Jorg Hockemeyer
    University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, Kreuzbergweg 26, D 53115 Bonn, Germany
    J Org Chem 69:3308-18. 2004
    ..57 microM). The light sensitivity of 8-styrylxanthine derivatives, not only in solution, but also in the solid state, has to be considered when using those compounds as pharmacological tools or drugs...
  42. ncbi request reprint Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative
    Stefan Kehraus
    Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, D 53115 Bonn, Germany
    J Med Chem 47:2243-55. 2004
    ..It was found that this ligand fit well into the binding pockets of both receptor subtypes because of its highly flexible structure, although in somewhat different binding modes...
  43. ncbi request reprint Improving potency, selectivity, and water solubility of adenosine A1 receptor antagonists: xanthines modified at position 3 and related pyrimido[1,2,3-cd]purinediones
    Stefanie Weyler
    University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, Kreuzbergweg 26, 53115 Bonn, Germany
    ChemMedChem 1:891-902. 2006
    ..Their efficacy was generally lower than that of the full inverse agonist DPCPX, and depended on subtle structural changes. Some of the new compounds belong to the most potent and selective A(1) antagonists described to date...
  44. ncbi request reprint Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors
    Ali El-Tayeb
    Pharmaceutical Chemistry I, Pharmaceutical Institute, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    J Med Chem 49:7076-87. 2006
    ....
  45. ncbi request reprint Synthesis and pharmacology of pyrido[2,3-d]pyrimidinediones bearing polar substituents as adenosine receptor antagonists
    Jacek Bulicz
    Department of Pharmaceutical Chemistry, Pharmaceutical Institute, University of Kiel, Gutenbergstrasse 76, D 24118 Kiel, Germany
    Bioorg Med Chem 14:2837-49. 2006
    ..3 nM, Ki human A1=153 nM, and Ki human A3>10,000 nM)...
  46. ncbi request reprint Development and validation of a capillary electrophoresis method for the characterization of herpes simplex virus type 1 (HSV-1) thymidine kinase substrates and inhibitors
    Jamshed Iqbal
    Pharmaceutical Institute, Department of Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Kreuzbergweg 26, D 53115 Bonn, Germany
    J Chromatogr B Analyt Technol Biomed Life Sci 846:281-90. 2007
    ..Phosphorylated products eluted within less than 7 min. The limits of detection were 0.36 microM for dTMP and 0.86 microM for GMP. The method was used to study enzyme kinetics, and to investigate alternative substrates and inhibitors...
  47. ncbi request reprint Development of off-line and on-line capillary electrophoresis methods for the screening and characterization of adenosine kinase inhibitors and substrates
    Jamshed Iqbal
    Department of Pharmaceutical Chemistry Poppelsdorf, Pharmaceutical Institute, University of Bonn, Bonn, Germany
    Electrophoresis 27:2505-17. 2006
    ..Dose-response curves and calculated K(i) values for standard antagonists obtained by CE were in excellent agreement with data obtained by the standard radioactive assay...
  48. doi request reprint Homology modelling of the human adenosine A2B receptor based on X-ray structures of bovine rhodopsin, the beta2-adrenergic receptor and the human adenosine A2A receptor
    Farag F Sherbiny
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, Bonn, Germany
    J Comput Aided Mol Des 23:807-28. 2009
    ..The new, validated A2B receptor model may serve as a basis for developing more potent and selective drugs...
  49. ncbi request reprint Extracellular metabolism of nucleotides in neuroblastoma x glioma NG108-15 cells determined by capillary electrophoresis
    Marko Kaulich
    Department of Pharmaceutical Chemistry Poppelsdorf, Pharmaceutical Institute, University of Bonn, Bonn, Germany
    Cell Mol Neurobiol 23:349-64. 2003
    ..5. Dipyridamole, which is a therapeutically used nucleoside reuptake inhibitor in humans, reduced the extracellular adenosine accumulation possibly by allosteric enhancement of adenosine reuptake into the cells...
  50. ncbi request reprint Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors
    Ali El-Tayeb
    Pharmaceutical Institute, Pharmaceutical Sciences Bonn PSB, University of Bonn, Kreuzbergweg 26, D 53115 Bonn, Germany
    Bioorg Med Chem Lett 15:5450-2. 2005
    ..57nM. Human platelets had a high density of P2Y(12) receptors exhibiting a B(max) value of 7.66pmol/mg of protein...
  51. doi request reprint A highly sensitive CE-UV method with dynamic coating of silica-fused capillaries for monitoring of nucleotide pyrophosphatase/phosphodiesterase reactions
    Jamshed Iqbal
    Pharmaceutical Sciences Bonn, Pharmaceutical Chemistry I, University of Bonn, Bonn, Germany
    Electrophoresis 29:3685-93. 2008
    ..The new method was used to study enzyme kinetics and inhibitors. It opens an easy way to determine the activities of slowly metabolizing enzymes such as NPPs, which are of considerable interest as novel drug targets...
  52. doi request reprint Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling
    Petra Hillmann
    PharmaCenter Bonn, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany
    J Med Chem 52:2762-75. 2009
    ..The disulfide bridge Cys25-Cys278 was found to be important for agonist potency but neither for agonist efficacy nor for antagonist potency...
  53. ncbi request reprint Binding of [3H]MSX-2 (3-(3-hydroxypropyl)-7-methyl-8-(m-methoxystyryl)-1-propargylxanthine) to rat striatal membranes--a new, selective antagonist radioligand for A(2A) adenosine receptors
    C E Muller
    Pharmaceutical Institute, Universitat Bonn, Germany
    Eur J Pharm Sci 10:259-65. 2000
    ..The new radioligand shows high specific radioactivity (85 Ci/mmol, 3150 GBq/mmol) and acceptable nonspecific binding at rat striatal membranes of 20-30%, at 1 nM...
  54. ncbi request reprint Rapid microwave-assisted fluorination yielding novel 5'-deoxy-5'-fluorouridine derivatives
    H Phuoc Le
    Pharmaceutical Sciences Bonn PSB, Pharmaceutical Chemistry, Institute of Pharmacy, University of Bonn, Kreuzbergweg 26, 53115 Bonn, Germany
    Bioorg Med Chem Lett 16:6139-42. 2006
    ..Nucleophilic substitution at the 5'-position of the nucleosides was achieved within 45 min providing excellent yields of 75-92% by application of microwaves...
  55. doi request reprint Development of a microbioreactor with ecto-nucleoside triphosphate diphosphohydrolase 2 (NTPDase2) immobilized on a polyacrylamide-coated capillary at the outlet
    Jamshed Iqbal
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    J Chromatogr A 1217:600-4. 2010
    ..The developed outlet immobilized enzyme microreactor using a coated capillary is very fast, simple and most economic allowing multiple use of the enzyme...
  56. doi request reprint Nucleoside-5'-monophosphates as prodrugs of adenosine A2A receptor agonists activated by ecto-5'-nucleotidase
    Ali El-Tayeb
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    J Med Chem 52:7669-77. 2009
    ..Compound 12g will be a new lead structure for the development of more potent and selective ecto-5'-NT-activated prodrugs of selective anti-inflammatory A(2A) receptor agonists...
  57. doi request reprint Synthesis of uracil nucleotide analogs with a modified, acyclic ribose moiety as P2Y(2) receptor antagonists
    Roland Sauer
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    Bioorg Med Chem 17:5071-9. 2009
    ....
  58. doi request reprint Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists
    Andrea Behrenswerth
    PharmaCenter Bonn, University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D 53121 Bonn, Germany
    Bioorg Med Chem 17:2842-51. 2009
    ..In further GTPgammaS binding studies selected compounds were shown to be antagonists or inverse agonists...
  59. ncbi request reprint Antinociceptive effects of novel A2B adenosine receptor antagonists
    Osama M Abo-Salem
    Laboratory of Molecular Neurobiology, Department of Psychiatry, University of Bonn, Bonn, Germany
    J Pharmacol Exp Ther 308:358-66. 2004
    ..Our results indicate that analgesic effects of caffeine are mediated, at least in part, by A2B adenosine receptors...
  60. ncbi request reprint Catalyst-free microwave-assisted amination of 2-chloro-5-nitrobenzoic acid
    Younis Baqi
    Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, D 53121 Bonn, Germany
    J Org Chem 72:5908-11. 2007
    ..Up to >99% isolated yield was obtained within 5-30 min at 80-120 degrees C. The reaction, which is suitable for upscaling, yielded new compounds that are of considerable interest as useful building blocks and as potential drugs...
  61. ncbi request reprint Capillary electrophoresis-based nanoscale assays for monitoring ecto-5'-nucleotidase activity and inhibition in preparations of recombinant enzyme and melanoma cell membranes
    Jamshed Iqbal
    Pharmaceutical Sciences Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, D 53121 Bonn, Germany
    Anal Biochem 373:129-40. 2008
    ..The CE methods were used for measuring enzyme kinetics and for assaying inhibitors and substrates. In addition, the online assay was successfully applied to melanoma cell membrane preparations natively expressing the human ecto-5'-NT...
  62. ncbi request reprint P2 receptors activated by uracil nucleotides--an update
    Andreas Brunschweiger
    Pharmaceutical Institute, University of Bonn, Bonn, Germany
    Curr Med Chem 13:289-312. 2006
    ..This article is an updated version of "P2-Pyrimidinergic Receptors and Their Ligands" by C. E. Müller published in Curr. Pharm. Des. 2002, 8, 2353-2369...
  63. ncbi request reprint Fast, efficient capillary electrophoresis method for measuring nucleotide degradation and metabolism
    Ramatullah Qurishi
    Department of Pharmaceutical Chemistry Poppelsdorf, Pharmaceutical Institute, University of Bonn, Germany
    J Chromatogr A 952:275-81. 2002
    ..Furthermore, we used the new method for monitoring enzymatic studies using the enzyme hexokinase to convert nucleotide triphosphates to diphosphates...
  64. ncbi request reprint [The medicinal chemistry of diuretics]
    Andreas Brunschweiger
    Pharmazeutisches Institut, Pharmazeutische Chemie Poppelsdorf, Bonn
    Pharm Unserer Zeit 35:310-20. 2006
  65. ncbi request reprint Ammonium-induced calcium mobilization in 1321N1 astrocytoma cells
    Petra Hillmann
    Pharmaceutical Sciences Bonn PSB, Pharmaceutical Chemistry I, Pharmaceutical Institute, University of Bonn, Bonn, Germany
    Toxicol Appl Pharmacol 227:36-47. 2008
    ..Our findings may contribute to the understanding of pathologic ammonium effects in different brain cells, and to the treatment of hyperammonemia...
  66. ncbi request reprint Blocking striatal adenosine A2A receptors: a new strategy for basal ganglia disorders
    Christa E Muller
    Pharmaceutical Institute, University of Bonn, Germany
    Recent Pat CNS Drug Discov 2:1-21. 2007
    ..Furthermore, the different chemical classes of A(2A) receptor antagonists that have been described in the literature, including recent patent literature, will be presented...
  67. pmc Adenosine regulates CD8 T-cell priming by inhibition of membrane-proximal T-cell receptor signalling
    Carsten Linnemann
    Institute for Molecular Medicine and Experimental Immunology, Friedrich Wilhelms University Bonn, Bonn, Germany
    Immunology 128:e728-37. 2009
    ..These data raise the possibility that extracellular adenosine has a physiological role in the regulation of CD8 T-cell priming and differentiation in peripheral organs...