Synthesis and pharmacology of a prohormone angiotensin antagonist.
A prohormone angiotensin antagonist, Sarcosyl1-Alanyl8-angiotensin I (Sar1-Ala8-A-I) was synthesized and its pharmacological properties were evaluated in three biological systems. It was found to be a good inhibitor in vivo in the rat blood pressure assay, somewhat less active in guinea pig ileum and a relatively weak antagonist in rat uterus. In vivo the inhibitory effect was greatly attenuated by the presence of the converting enzyme inhibitor BPP5alpha.
D000803:Angiotensin I / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000138:chemical synthesis; D000804:Angiotensin II / Q000037:antagonists & inhibitors*; D000809:Angiotensins; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D051381:Rats; D012504:Saralasin / Q000494:pharmacology; D014590:Uterine Contraction / Q000187:drug effects
D000809:Angiotensins; D000804:Angiotensin II; D000803:Angiotensin I; D012504:Saralasin