| 摘要 |
PURPOSE:To obtain an endothelin inhibitor by using a compound having excellent endothelin antagonistic action and action to suppress the increase of intracellular calcium concentration as an active component. CONSTITUTION:A compound of formula I (R<1> is group of formula II, formula III, etc. ; R<2> and R<3> together form a single bond or R<2> is H and R<3> is group of formula IV) is used as an active component. The compound of formula I can be produced by culturing a microorganism belonging to the genus Streptomyces (e.g. Streptomyces sp. RE-1241 strain) in a medium and separating and purifying the compound produced and accumulated in the culture product. It can be formed in the form of oral or parenteral drug and the daily administration dose is 0.01-2mg/kg for adult. It is useful for the treatment of hypertension, asthma, cerebral apoplexy, acute renal insufficiency, myocardial infarction, stenocardia, cerebrovascular spasm, etc. |
