An angiotensin II antagonist with strongly prolonged action.
A highly hydrophobic analogue of angiotensin II (AT), [Sar1,(2',3',4',5',6'-Br5)Phe8]AT exhibited strong and persistent specific antagonism against AT, both in vitro and in vivo. This peptide exhibited 32% of the binding affinity of [Sar1]AT towards membranes of bovine adrenal cortex, it was a specific AT antagonist of irreversible character on smooth muscle assays, and it also suppressed for over 120 min at 7.10(-8) M/kg the blood pressure response towards AT in the rat blood pressure assay. This compound harbours therefore the potential of a new class of AT-specific antihypotensive drugs.
Holck
M
M
Hoffmann La Roche A.G., Basel, Switzerland.
Bossé
R
R
Fischli
W
W
Gerold
H
H
Escher
E
E
D000302:Adrenal Cortex / Q000187:drug effects / Q000378:metabolism; D000804:Angiotensin II / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors* / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D001667:Binding, Competitive; D001794:Blood Pressure / Q000187:drug effects; D002417:Cattle; D002462:Cell Membrane / Q000378:metabolism; D005260:Female; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D009119:Muscle Contraction / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012504:Saralasin / Q000494:pharmacology; D013237:Stereoisomerism
D000804:Angiotensin II; C009210:sarleucin; C059928:angiotensin-II, Sar-Arg-Val-Tyr-Val-His-Pro-(2',3',4',5',6'-pentabromo)-Phe; D012504:Saralasin