• Title of article

    8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor antagonists Original Research Article

  • Author/Authors

    Christa E. Müller-Sieburg، نويسنده , , Jes?s Sandoval-Ram??rez، نويسنده , , Ulrike Schobert، نويسنده , , Uli Geis، نويسنده , , Wolfram Frobenius، نويسنده , , Karl-Norbert Klotz، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 1998
  • Pages
    13
  • From page
    707
  • To page
    719
  • Abstract
    8-(Sulfostyryl)xanthine derivatives were synthesized as water-soluble A2A-selective adenosine receptor (AR) antagonists. meta- and para-sulfostyryl-DMPX (3,7-dimethyl-1-propargylxanthine) derivatives 11a and 11b exhibited high affinity to rat A2A-AR in submicromolar concentrations, and were 20- to 30-fold selective versus rat A1-AR. Styryl-DMPX derivatives were inactive at human A2B- and A3-AR. 1,3-Dipropyl-8-p-sulfostyrylxanthine (13) and its 7-methyl derivative (14) showed similar (13) or higher (14) A2A affinity than 11a and 11b but showed no (13) or only a low degree (14) of selectivity versus A1-, A2B-, and A3-AR. The A2A-selective sulfostyryl-DMPX derivatives exhibit high water-solubility and may be useful research tools for in vivo studies.
  • Keywords
    Sulfonic acids , A2B- , Xanthines , A2A- , A1- , A3-adenosine receptors , A2A-antagonists , Water-solubility
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Serial Year
    1998
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Record number

    1301552

    • Link To Document
    https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=1301552