• Title of article

    N-Methylbenzanilide derivatives as a novel class of selective V1A receptor antagonists

  • Author/Authors

    Akio Kakefuda، نويسنده , , Junko Tsukada، نويسنده , , Toshiyuki Kusayama، نويسنده , , Atsuo Tahara، نويسنده , , Shin-ichi Tsukamoto، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2002
  • Pages
    4
  • From page
    229
  • To page
    232
  • Abstract
    During our efforts to develop a novel class of selective V1A receptor antagonists, the N-methylbenzanilide structure was applied to a 4,4-difluoro-1-benzazepine derivative, 4, which is a selective V1A receptor antagonist. Further structural modifications gave 16a with high V1A affinity and V2/V1A selectivity (Ki=5.71 nM, V2/V1A=140) and potent V1A receptor antagonist activity (ID50=0.0080 mg/kg iv).
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2002
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    791942