C R Ganellin

Summary

Affiliation: University College London
Country: UK

Publications

  1. doi request reprint Personal reflections on Sir James Black (1924-2010) and histamine
    C Robin Ganellin
    Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H 0AJ, UK
    Inflamm Res 60:103-10. 2011
  2. ncbi request reprint Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors
    C Robin Ganellin
    Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, England
    J Med Chem 48:7333-42. 2005
  3. ncbi request reprint University education of medicinal chemists: comparison of eight countries
    C R Ganellin
    Department of Chemistry, The Christopher Ingold Laboratories, University College London, 20 Gordon Street, London, UK
    Eur J Med Chem 35:163-74. 2000
  4. ncbi request reprint Synthesis and structure-activity relationships of dequalinium analogues as K+ channel blockers. Investigations on the role of the charged heterocycle
    D Galanakis
    Department of Chemistry, University College London, U K
    J Med Chem 38:595-606. 1995
  5. ncbi request reprint Synthesis and quantitative structure-activity relationships of dequalinium analogues as K+ channel blockers: investigation into the role of the substituent at position 4 of the quinoline ring
    D Galanakis
    Department of Chemistry, University College London, UK
    J Med Chem 38:3536-46. 1995
  6. ncbi request reprint Synthesis and quantitative structure-activity relationship of a novel series of small conductance Ca(2+)-activated K+ channel blockers related to dequalinium
    D Galanakis
    Department of Chemistry, University College London, UK
    J Med Chem 39:359-70. 1996
  7. ncbi request reprint Inhibitors of tripeptidyl peptidase II. 2. Generation of the first novel lead inhibitor of cholecystokinin-8-inactivating peptidase: a strategy for the design of peptidase inhibitors
    C R Ganellin
    Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, England
    J Med Chem 43:664-74. 2000
  8. ncbi request reprint Synthesis and pharmacological testing of dequalinium analogues as blockers of the apamin-sensitive Ca(2+)-activated K+ channel: variation of the length of the alkylene chain
    D Galanakis
    Department of Chemistry, University College London, U K
    J Med Chem 39:3592-5. 1996
  9. pmc Enhancement of hippocampal pyramidal cell excitability by the novel selective slow-afterhyperpolarization channel blocker 3-(triphenylmethylaminomethyl)pyridine (UCL2077)
    Mala M Shah
    Department of Pharmacology, University College London, Gower Street, London WC1E 6BT UK
    Mol Pharmacol 70:1494-502. 2006
  10. ncbi request reprint Tritylamino aromatic heterocycles and related carbinols as blockers of ca 2+-activated potassium ion channels underlying neuronal hyperpolarization
    Patricia A Zunszain
    Department of Chemistry, University College London, 20 Gordon Street, UK
    Arch Pharm (Weinheim) 335:159-66. 2002

Collaborators

  • P M Dunn
  • Saad Al-Damluji
  • Mala M Shah
  • O Lafont
  • Lihua Zhao
  • Alessandro Piergentili
  • Sven Grassmann
  • Dimitrios Galanakis
  • Jean Charles Schwartz
  • Xavier Ligneau
  • Holger Stark
  • Walter Schunack
  • Jean Michel Arrang
  • Antonios Dougalis
  • Galina Meier
  • Heinz H Pertz
  • Joaquim Fernando Mendes da Silva
  • David I Fletcher
  • Eoin C Power
  • George Lees
  • Nadia Pelloux-Léon
  • Tibor Mikó
  • Astrid Sasse
  • Patricia A Zunszain
  • Joachim Apelt
  • Marcus Walters
  • Donald H Jenkinson
  • David C H Benton
  • Antonia Piripitsi
  • Annette Hüls
  • Abdellatif Fkyerat
  • Michael Krause
  • Monique Garbarg
  • Wasyl Tertiuk
  • Agnès Rouleau
  • Sigurd Elz
  • J Campos Rosa
  • Mazyar Javadzadeh-Tabatabaie
  • Zena Miscony
  • Dennis G Haylett

Detail Information

Publications27

  1. doi request reprint Personal reflections on Sir James Black (1924-2010) and histamine
    C Robin Ganellin
    Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H 0AJ, UK
    Inflamm Res 60:103-10. 2011
    ..The characterisation of a second type of histamine receptor revitalised interest in histamine and led to many later studies on the role of histamine in inflammation...
  2. ncbi request reprint Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors
    C Robin Ganellin
    Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, England
    J Med Chem 48:7333-42. 2005
    ..4 microM. Molecular modeling, to determine the minimum energy conformations and explain the 1000-fold better affinity of butabindide, indicated that 37 cannot access the likely active conformation of butabindide...
  3. ncbi request reprint University education of medicinal chemists: comparison of eight countries
    C R Ganellin
    Department of Chemistry, The Christopher Ingold Laboratories, University College London, 20 Gordon Street, London, UK
    Eur J Med Chem 35:163-74. 2000
    ..The evidence suggests that academic training of medicinal chemists equips them to enter a wide range of occupations, many of which are in industry...
  4. ncbi request reprint Synthesis and structure-activity relationships of dequalinium analogues as K+ channel blockers. Investigations on the role of the charged heterocycle
    D Galanakis
    Department of Chemistry, University College London, U K
    J Med Chem 38:595-606. 1995
    ..However, among the heterocycles studied, quinoline is optimal. Furthermore, charge delocalization seems to be important: the higher the degree of delocalization the more potent the compound...
  5. ncbi request reprint Synthesis and quantitative structure-activity relationships of dequalinium analogues as K+ channel blockers: investigation into the role of the substituent at position 4 of the quinoline ring
    D Galanakis
    Department of Chemistry, University College London, UK
    J Med Chem 38:3536-46. 1995
    ..This is consistent with simple charge transfer from the channel to the blocker and may refer to other processes which are important for the strength of the drug-K+ channel interaction such as the desolvation of the compounds...
  6. ncbi request reprint Synthesis and quantitative structure-activity relationship of a novel series of small conductance Ca(2+)-activated K+ channel blockers related to dequalinium
    D Galanakis
    Department of Chemistry, University College London, UK
    J Med Chem 39:359-70. 1996
    ..17(+/-0.15)ELUMO +5.33(+/-0.76)(n =24, r = 0.85, s = 0.249)]. A possible physical meaning for the ELUMO correlation based upon the principle of maximum hardness is discussed...
  7. ncbi request reprint Inhibitors of tripeptidyl peptidase II. 2. Generation of the first novel lead inhibitor of cholecystokinin-8-inactivating peptidase: a strategy for the design of peptidase inhibitors
    C R Ganellin
    Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, England
    J Med Chem 43:664-74. 2000
    ..The strategy for this work is explicitly described since it illustrates a possible general approach for peptidase inhibitor design...
  8. ncbi request reprint Synthesis and pharmacological testing of dequalinium analogues as blockers of the apamin-sensitive Ca(2+)-activated K+ channel: variation of the length of the alkylene chain
    D Galanakis
    Department of Chemistry, University College London, U K
    J Med Chem 39:3592-5. 1996
    ..These results are discussed in the context of possible modes of binding of the compounds to the SKCa channel...
  9. pmc Enhancement of hippocampal pyramidal cell excitability by the novel selective slow-afterhyperpolarization channel blocker 3-(triphenylmethylaminomethyl)pyridine (UCL2077)
    Mala M Shah
    Department of Pharmacology, University College London, Gower Street, London WC1E 6BT UK
    Mol Pharmacol 70:1494-502. 2006
    ....
  10. ncbi request reprint Tritylamino aromatic heterocycles and related carbinols as blockers of ca 2+-activated potassium ion channels underlying neuronal hyperpolarization
    Patricia A Zunszain
    Department of Chemistry, University College London, 20 Gordon Street, UK
    Arch Pharm (Weinheim) 335:159-66. 2002
    ..1-1.2 microM) and are much more selective than clotrimazole since they have less effect on the high voltage-activated Ca2+ current...
  11. ncbi request reprint Synthesis and pharmacological testing of polyaminoquinolines as blockers of the apamin-sensitive Ca2+-activated K+ channel (SK(Ca))
    David I Fletcher
    Department of Chemistry, University College London, 20, Gordon Street, London WC1H 0AJ, UK
    Bioorg Med Chem 15:5457-79. 2007
    ..13-0.36 microM). Extension to four aminoquinoline residues increased the potency to IC(50)=93 nM...
  12. ncbi request reprint Synthesis, molecular modeling, and K+ channel-blocking activity of dequalinium analogues having semirigid linkers
    J Campos Rosa
    Department of Chemistry, University College London, U K
    J Med Chem 39:4247-54. 1996
    ..These two factors may permit favorable contacts between the quinolinium groups and the channel over a range of intramolecular separations...
  13. doi request reprint Molecular features of the prazosin molecule required for activation of Transport-P
    Joaquim Fernando Mendes da Silva
    Department of Chemistry, Christopher Ingold Laboratories, University College London, 20 Gordon Street, London WC1H 0AJ, UK
    Bioorg Med Chem 16:7254-63. 2008
    ..It is shown that the structure of prazosin appears to be very specific for the activation. Only quinazolines have been found to activate, and the presence of the 6,7-dimethoxy and 4-amino groups appears to be critically important...
  14. ncbi request reprint Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca))
    Eoin C Power
    Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, UK
    Bioorg Med Chem Lett 16:887-90. 2006
    ..The properties of the phenoxy moiety seem to determine whether the compounds act to open or block the channel...
  15. ncbi request reprint Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain
    Nadia Pelloux-Léon
    Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, England, UK
    J Med Chem 47:3264-74. 2004
    ....
  16. ncbi request reprint Defining determinant molecular properties for the blockade of the apamin-sensitive SKCa channel in guinea-pig hepatocytes: the influence of polarizability and molecular geometry
    Dimitrios Galanakis
    Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, 541 24 Thessaloniki, Greece
    Bioorg Med Chem Lett 14:4031-5. 2004
    ..The polarizability is not adequate to describe the potency of the most potent blockers with a good stereochemical fit to the channel, presumably due to more specific interactions taking place...
  17. ncbi request reprint Search for histamine H(3) receptor ligands with combined inhibitory potency at histamine N-methyltransferase: omega-piperidinoalkanamine derivatives
    Sven Grassmann
    Institut fur Pharmazie, Institut fur Pharmazie, Berlin, Germany
    Arch Pharm (Weinheim) 337:533-45. 2004
    ..In this study, new hybrid compounds with a dual mode biological action were developed. These pharmacological agents are valuable leads for further development and candidates for treatment of histamine-dependent disorders...
  18. ncbi request reprint Bis-quinolinium cyclophanes: toward a pharmacophore model for the blockade of apamin-sensitive SKCa channels in sympathetic neurons
    Dimitrios Galanakis
    Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 541 24, Greece
    Bioorg Med Chem Lett 14:4231-5. 2004
    ..These are (i) an optimum distance of ca. 5.8A between the centroids of the pyridinium rings of the two quinolinium groups and (ii) a preference for conformations having the quinolinium groups in a synperiplanar orientation...
  19. ncbi request reprint 4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists
    Galina Meier
    Institut fur Pharmazie, Freie Universitat Berlin, Konigin Luise Strasse 2 4, 14195 Berlin, Germany
    J Med Chem 47:2678-87. 2004
    ..Additionally, selected compounds were functionally investigated in vitro on isolated organs of the guinea-pig at H(3), H(1), and H(2) receptors...
  20. ncbi request reprint The sleep lipid oleamide may represent an endogenous anticonvulsant: an in vitro comparative study in the 4-aminopyridine rat brain-slice model
    Antonios Dougalis
    Sunderland Pharmacy School, School of Health, Social and Natural Sciences, University of Sunderland, Wharncliffe Street, Sunderland, SR1 3SD, UK
    Neuropharmacology 46:541-54. 2004
    ..cOA does not possess profound antiepileptic actions in our hands compared to CBZ, PB or CRX...
  21. ncbi request reprint The sleep inducing brain lipid cis-oleamide (cOA) does not modulate serotonergic transmission in the CA1 pyramidal neurons of the hippocampus in vitro
    Antonios Dougalis
    Sunderland Pharmacy School, School of Health, Social and Natural Sciences, University of Sunderland, Chester Road Campus, Wharncliffe Street, Sunderland, SR1 3SD, UK
    Neuropharmacology 46:63-73. 2004
    ..In summary, cis-oleamide failed to modulate metabotropic responses to exogenous 5-HT in this microelectrode study at concentrations well in excess of those reported to modulate 5-HT1A and 5-HT2A/C systems in earlier studies...
  22. ncbi request reprint Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds
    Tibor Mikó
    Institut fur Pharmazie, Freie Universitat Berlin, Konigin Luise Strasse 2 4, Germany
    J Med Chem 46:1523-30. 2003
    ..Unexpectedly, some of the novel antagonists also showed a slight preference for the human histamine H(3) receptor compared to their affinities for the guinea-pig H(3) receptor...
  23. ncbi request reprint Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties
    Astrid Sasse
    Institut fur Pharmazie, Freie Universitat Berlin, Konigin Luise Strasse 2 4, 14195 Berlin, Germany
    J Med Chem 45:4000-10. 2002
    ..07-0.1 mg/kg depending on tissue)...
  24. ncbi request reprint Piperidino-hydrocarbon compounds as novel non-imidazole histamine H(3)-receptor antagonists
    Galina Meier
    Institut fur Pharmazie, Freie Universitat Berlin, Konigin Luise Strasse 2 4, 14195 Berlin, Germany
    Bioorg Med Chem 10:2535-42. 2002
    ..The ED(50) values for 9 and 10 were 1.3 and 1.4mg/kg po, respectively, which is in the potency range of the reference antagonist thioperamide...
  25. ncbi request reprint Progress in the proxifan class: heterocyclic congeners as novel potent and selective histamine H(3)-receptor antagonists
    Sven Grassmann
    Institut fur Pharmazie, Freie Universitat Berlin, Konigin Luise Strasse 2 4, 14195, Germany
    Eur J Pharm Sci 15:367-78. 2002
    ..Thus, these novel H(3)-receptor antagonists are interesting leads for further development...
  26. ncbi request reprint Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity
    Joachim Apelt
    Institut fur Pharmazie, Freie Universitat Berlin, Konigin Luise Strasse 2 4, 14195 Berlin, Germany
    J Med Chem 45:1128-41. 2002
    ....
  27. ncbi request reprint Imidazole derivatives as a novel class of hybrid compounds with inhibitory histamine N-methyltransferase potencies and histamine hH3 receptor affinities
    Sven Grassmann
    Institut fur Pharmazie, Freie Universitat Berlin, Konigin Luise Strasse 2 4, 14195 Berlin, Germany
    Bioorg Med Chem 11:2163-74. 2003
    ..The most interesting compound (14) is simultaneously a highly potent H(3) receptor ligand (K(i)=4.1nM) and a highly potent HMT inhibitor (IC(50)=24nM), which makes this derivative a valuable pharmacological tool for further development...