Why the study?
Does [Sar(1), Ile(8)]-angiotensin II have a more potent and long-lasting competitive antagonistic effect against angiotensin II compared to [Ile(8)]-angiotensin II in isolated rabbit aorta and anesthetized cats and dogs?
Does [Sar(1), Ile(8)]-angiotensin II have a more potent and long-lasting competitive antagonistic effect against angiotensin II compared to [Ile(8)]-angiotensin II in isolated rabbit aorta and anesthetized cats and dogs?
The modification of angiotensin II at positions 1 and 8 creates a potent, long-lasting competitive inhibitor in vivo, likely due to protection against enzymatic degradation.
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May guide design of longer-acting angiotensin antagonists; leaves open translation to human cardiovascular therapeutics.
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.
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Türker et al. (1972) studied this question.
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