WS-7338, new endothelin receptor antagonists isolated from Streptomyces sp. No. 7338. II. Biological characterization and pharmacological characterization of WS-7338 B

J Antibiot (Tokyo). 1992 Jan;45(1):83-7. doi: 10.7164/antibiotics.45.83.

Abstract

WS-7338, produced by Streptomyces sp. No. 7338, was found to be a competitive and specific antagonist against ET-1 receptors in in vitro studies and WS-7338 B is also active in vivo. Furthermore, WS-7338 B was a specific antagonist for vascular ET-1 receptors (ETA receptors) and significantly prevented the accumulation of intracellular inositol 1,4,5-triphosphate (IP3) in endothelin treated rat aorta tissues.

MeSH terms

  • Animals
  • Aorta / metabolism
  • Binding, Competitive
  • Brain / metabolism
  • Culture Techniques
  • Dose-Response Relationship, Drug
  • Endothelium, Vascular / metabolism*
  • Humans
  • Kidney / metabolism
  • Lung / metabolism
  • Male
  • Peptides, Cyclic / pharmacology*
  • Rabbits
  • Rats
  • Receptors, Cell Surface / antagonists & inhibitors*
  • Receptors, Endothelin
  • Swine

Substances

  • Peptides, Cyclic
  • Receptors, Cell Surface
  • Receptors, Endothelin
  • cyclo(glutamyl-alanyl-isoleucyl-leucyl-tryptophyl)