WS-7338, new endothelin receptor antagonists isolated from Streptomyces sp. No. 7338. II. Biological characterization and pharmacological characterization of WS-7338 B.
نویسندگان
چکیده
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.
منابع مشابه
Discovery of endothelin antagonists
Novel cyclic pentapeptides, WS7338A, B, C and D [cyclo-(AAl -AA2-DTrp-D-Glu-Ala)] were isolated as Endothelin (ET) receptor antagonists from the culture broth of Sfreptomyces sp. No. 7338. Based on conformational analysis of these seeds, we defined the minimum structural requirements for binding affinity and prepared a series of acylated tripeptides with ETA receptor binding affinity. Through e...
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عنوان ژورنال:
- The Journal of antibiotics
دوره 45 1 شماره
صفحات -
تاریخ انتشار 1992