| 摘要 |
Novel compounds according to aspects of this invention are provided by the modification of the sequence of the mammalian peptide hormone bradykinin (Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg) by the substitution of the L-Pro at position 7 in a unique manner which produces sequence-related analogues, i.e., hydroxyproline ethers or thioethers, that act as specific and competitive inhibitors of the biological activities of bradykinin to convert bradykinin agonists into bradykinin antagonists. Pharmaceutically-acceptable salts thereof, and compositions containing them are also provided. These compounds are useful in the treatment of various diseases including inflammatory disorders, asthma, septic shock and burn pain, for example, where an excess of bradykinin or related kinins are produced or injected, e.g., by insect bites.
|
