| abstract |
An endothelin-antagonizing peptide compound represented by general formula (I) and a pharmacologically acceptable salt thereof: R¹-R²-R³-R⁴-R⁵-R⁶-R⁷-R⁸-R⁹-R¹⁰-R¹¹-R¹²-Phe-R¹⁴-R¹⁵-R¹⁶-R¹⁷-R¹⁸-Ile-R²⁰-Z wherein R¹ is X¹-Gly, X³(a), X²-SCH₂CO or hydrogen; R² is Asn, Asp, Phe, Tyr, Ser or a single bond; R³ is Trp, Ile, Pro, Ala or a single bond; R⁴ is His, Lys, Gly, Trp, Ala or a single bond; R⁵ is Gly, Thr, Trp, Val or a single bond; R⁶ is Gly, Thr, Asn, Tyr, Asp or a single bond; R⁷ is Ala, Ser, Asn, Asp, Tyr, Phe or a single bond; R⁸ is Pro, Ala, Arg or a single bond; R⁹ is (b), (c) or a single bond; R¹⁰ is Trp or Ala; R¹¹ is Val, Pro or a single bond; R¹² is Tyr or a single bond; R¹⁴ is Ala, MeAla, Ser or Cys; R¹⁵ is His or Trp; R¹⁶ is Leu or Nva; R¹⁷ is Asp, Thr, Asn, Ser, Gly or Glu; R¹⁸ is Ile, Leu, Cha, Abu, Thi, Met, Tyr, MeLeu, MeIle, Phg or Nle; R²⁰ is Trp, Phe or Tyr; and Z is hydroxy, lower alkoxy or amino. |