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)