A new, long-lasting competitive inhibitor of angiotensin.
An analog of angiotensin II, [Sar(1), Ile(8)]-angiotensin II, has a potent and long-lasting competitive antagonistic effect against angiotensin II when tested for its myotropic action on the isolated rabbit aorta and for its effect on blood pressure in anesthetized cats and dogs. Compared to [Ile(8)]-angiotensin II, the new analog has equal antagonistic potency on the isolated system but a much greater potency in vivo. It is assumed that sarcosine in position 1 protects the peptide against enzymatic degradation and enhances its half-life. This study demonstrates that the modification in both positions 1 and 8 are important for the in vivo antagonistic potencies of angiotensin analogs.
D000804:Angiotensin II / Q000008:administration & dosage / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D000818:Animals; D001011:Aorta / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D002415:Cats; D004285:Dogs; D066298:In Vitro Techniques; D007275:Injections, Intravenous; D007532:Isoleucine / Q000494:pharmacology; D011817:Rabbits; D012521:Sarcosine / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013997:Time Factors
D007532:Isoleucine; D000804:Angiotensin II; D012521:Sarcosine