Pharmacological Characterization of the Novel Histamine H3-Receptor Antagonist N-(3,5-Dichlorophenyl)-N′-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687)

  title={Pharmacological Characterization of the Novel Histamine H3-Receptor Antagonist N-(3,5-Dichlorophenyl)-N′-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687)},
  author={Robbie L Mcleod and Charles A. Rizzo and Robert E. West and Robert. Aslanian and Kevin D. Mccormick and Matthew S. Bryant and Yunsheng Hsieh and Walter A. Korfmacher and Garfield G. Mingo and Lori A. Varty and Shirley M. Williams and Nengyang Shih and Robert W. Egan and John A. Hey},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={1037 - 1044}
  • R. Mcleod, C. Rizzo, J. Hey
  • Published 1 June 2003
  • Biology, Chemistry, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
We present the pharmacological and pharmacokinetic profiles of a novel histamine H3 receptor antagonist, N-(3,5-dichlorophenyl)-N′-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687). The H3-receptor binding Ki values for SCH 79687 were 1.9 and 13 nM in the rat and guinea pig (GP), respectively. The Ki values for SCH 79687 at histamine H1 and H2 receptors were greater than 1 μM. SCH 79687 showed a 41- and 82-fold binding selectivity for the H3 receptor over α2A-adrenoceptors and… 

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