title: WS-7338, new endothelin receptor antagonists isolated from Streptomyces sp. No. 7338. II. Biological characterization and pharmacological characterization of WS-7338 B.
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.
authors.affiliation: Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Miyata
authors.forename: M
authors.initials: M
authors.lastname: Hashimoto
authors.forename: K
authors.initials: K
authors.lastname: Fujie
authors.forename: M
authors.initials: M
authors.lastname: Nishikawa
authors.forename: S
authors.initials: S
authors.lastname: Kiyoto
authors.forename: M
authors.initials: M
authors.lastname: Okuhara
authors.forename: M
authors.initials: M
authors.lastname: Kohsaka
mesh_terms: D000818:Animals; D001011:Aorta / Q000378:metabolism; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D046508:Culture Techniques; D004305:Dose-Response Relationship, Drug; D004730:Endothelium, Vascular / Q000378:metabolism*; D006801:Humans; D007668:Kidney / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D008297:Male; D010456:Peptides, Cyclic / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors*; D017466:Receptors, Endothelin; D013552:Swine
chemical_list: D010456:Peptides, Cyclic; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin; C069764:cyclo(glutamyl-alanyl-isoleucyl-leucyl-tryptophyl)