Key result
Oral AT1 antagonist KR-30988 shows greater anti-hypertensive potency than losartan in animal models.
Why the study?
The pharmacological profile and potency of KR-30988, a novel non-peptide AT1 receptor antagonist, required characterization in various experimental models.
Population
In-vitro recombinant human AT1/AT2 receptors, rat and rabbit aorta; in-vivo pithed rats, conscious renal hypertensive rats, conscious furosemide-treated dogs
Comparison
KR-30988 versus losartan
Design
Preclinical pharmacological study
Authors
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May support preclinical development of KR-30988; leaves open clinical translation and therapeutic utility.
KR-30988 is a potent, orally active, selective AT1 receptor antagonist with insurmountable antagonism in preclinical models.
Lee et al. (1999) studied Hypertension (animal models). KR-30988 vs. Losartan was evaluated. KR-30988 is a potent, orally active selective AT1 receptor antagonist with insurmountable antagonism, demonstrating greater anti-hypertensive potency than losartan in animal models.
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