RES-1149-1 AND-2, NOVEL NONPEPTIDIC ENDOTHELIN TYPE-B RECEPTOR ANTAGONISTS PRODUCED BY ASPERGILLUS SP .3. BIOCHEMICAL-PROPERTIES OF RES-1149-1,-2 AND STRUCTURE-ACTIVITY-RELATIONSHIPS

Authors
OGAWA T UOSAKI Y TANAKA T TSUKUDA E MIHARA A MATSUDA Y
Citation
T. Ogawa et al., RES-1149-1 AND-2, NOVEL NONPEPTIDIC ENDOTHELIN TYPE-B RECEPTOR ANTAGONISTS PRODUCED BY ASPERGILLUS SP .3. BIOCHEMICAL-PROPERTIES OF RES-1149-1,-2 AND STRUCTURE-ACTIVITY-RELATIONSHIPS, Journal of antibiotics, 49(2), 1996, pp. 168-172
Citations number
13
Categorie Soggetti
Pharmacology & Pharmacy",Immunology,"Biothechnology & Applied Migrobiology
Journal title
Journal of antibiotics → ACNP
ISSN journal
00218820
Volume
49
Issue
2
Year of publication
1996
Pages
168 - 172
Database
ISI
SICI code
0021-8820(1996)49:2<168:RANNET>2.0.ZU;2-0
Abstract
RES-1149-1 and -2, produced by Aspergillus sp. RE-1149, were found to be non-peptidic antagonists for endothelin type B receptor (ET(B) rece ptor). RES-1149-1 and -2 selectively inhibited the endothelin-1 (ET-1) binding to ET(B) receptor in a competitive manner with IC50 values of 1.5 mu M and 20 mu M, respectively. RES-1149-1 inhibited the increase in intracellular Ca2+ concentration elicited by 1 nM ET-1 in COS-7 te lls expressing human ET(B) receptor, but not in the case of cells expr essing ET(A) receptor. In addition, some structure-activity relationsh ips are described.