Bradykinin analogs containing alpha-aminoisobutyric acid (Aib).
All seven possible bradykinin (BK) analogs contained Aib in place of proline have been synthesized by the solid phase method and assayed for in vitro myotropic activity on the guinea pig ileum and rat uterus, and in vivo on the rat blood pressure, both in intravenous and intra-aortic administration. [Aib(2,3)]-BK, [Aib(2,7)]-BK, and [Aib(2,3,7)]-BK had no in vivo or in vitro activities; [Aib(2)]-BK, [Aib(3)]-BK and [Aib(3,7)]-BK had moderate BK-like activities and a significantly increased resistance to pulmonary inactivation in the rat ([Aib(3,7)]-BK was totally resistant). [Aib(7)]-BK was found to be the most active position seven BK analog yet assayed on the rat blood pressure, and shows remarkably high ileum (4 times BK) and intravenous rat blood pressure (6 times BK) activity.
D000621:Aminoisobutyric Acids; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001920:Bradykinin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D007202:Indicators and Reagents; D009119:Muscle Contraction / Q000187:drug effects; D051381:Rats; D013329:Structure-Activity Relationship; D014590:Uterine Contraction / Q000187:drug effects
D000621:Aminoisobutyric Acids; D007202:Indicators and Reagents; D001920:Bradykinin