Key result
New nonpeptide angiotensin II receptor antagonists demonstrated up to a 1000-fold increase in binding affinity compared to literature leads, with IC50 values reaching 0.012 microM.
Population
In vitro binding assays for angiotensin II receptor
Comparison
Nonpeptide angiotensin II receptor antagonists vs Literature leads (including lead 1)
Design
Preclinical
Authors
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May enable oral AII blockade for hypertension; leaves open clinical efficacy and safety validation.
Effect estimate: 1000-fold increase in binding affinity
Absolute Event Rate: 0.012% vs 15%
The discovery of nonpeptide angiotensin II receptor antagonists with high binding affinity provides a new class of potent antihypertensive agents.
Duncia et al. (1990) studied Hypertension. Nonpeptide angiotensin II receptor antagonists vs. Literature leads was evaluated on Angiotensin II receptor binding affinity (IC50) (1000-fold increase in binding affinity). New nonpeptide angiotensin II receptor antagonists demonstrated up to a 1000-fold increase in binding affinity compared to literature leads, with IC50 values reaching 0.012 microM.
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