• Title of article

    Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists

  • Author/Authors

    Robert A. Daines، نويسنده , , Kelvin K. C. Sham، نويسنده , , Jack J. Taggart، نويسنده , , William D. Kingsbury، نويسنده , , James Chan، نويسنده , , Ann Breen، نويسنده , , Jyoti Disa، نويسنده , , Nambi Aiyar، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 1997
  • Pages
    4
  • From page
    2673
  • To page
    2676
  • Abstract
    A high-throughput screen identified quinine analog 1 as an antagonist of the human calcitonin generelated peptide (hCGRP) receptor. Thus, compound 1 displaces [125I]-CGRP from the hCGRP receptor and inhibits CGRP-mediated cAMP production with IC50 values of 5.9 ± 1.2 μM and 26 ± 5 μM, respectively. A limited structure-activity study of 1 is described.
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    1997
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    789025