FR-900452, a specific antagonist of platelet activating factor (PAF) produced by Streptomyces phaeofaciens. I. Taxonomy, fermentation, isolation, and physico-chemical and biological characteristics.

Authors:
  • MOMasanori Okamoto
    Masanori Okamoto
  • KYKeizo Yoshida
    Keizo Yoshida
  • MNMotoaki Nishikawa
    Motoaki Nishikawa
  • TATakeshi Ando
    Takeshi Ando
  • MIMorita Iwami
    Morita Iwami
  • MKMasanobu Kohsaka
    Masanobu Kohsaka
  • HAHatsuo Aoki
    Hatsuo Aoki

Abstract
A PAF antagonist, designated as FR-900452, was isolated from fermentation products of Streptomyces phaeofaciens and the molecular formula was determined as C22H25N3O3S. The compound inhibited PAF-induced rabbit platelet aggregation with an IC50 of 3.7 X 10(-7)M, but was much less active against collagen-, arachidonic acid- or ADP-induced aggregation (IC50; 6.4 X 10(-5), greater than 10(-4) or greater than 10(-4)M, respectively).