Key result
FK 739 is a potent, competitive AT1-receptor antagonist that dose-dependently reduced blood pressure in hypertensive animal models without enhancing capsaicin-induced bronchial edema.
Population
Preclinical models including rat aortic smooth muscle cell membrane, bovine cerebellum membrane, isolated…
Comparison
FK 739 administered in vitro or orally in vivo. vs Vehicle, DuP 753, captopril, or saralasin.
Design
Preclinical
Authors
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Preclinical BP reduction with FK 739 warrants human trials; leaves open whether it avoids bronchial effects in patients.
Effect estimate: IC50 8.6 nM
FK 739 is a potent and selective AT1-receptor antagonist that effectively lowers blood pressure in preclinical models without inducing bronchial edema associated with ACE inhibitors.
Hamada et al. (1993) studied Hypertension (preclinical models). FK 739 vs. Vehicle, DuP 753, captopril was evaluated on Inhibition of specific binding of [125I]-angiotensin II to rat aortic smooth muscle cell membrane (IC50 8.6 nM). FK 739 is a potent, competitive AT1-receptor antagonist that dose-dependently reduced blood pressure in hypertensive animal models without enhancing capsaicin-induced bronchial edema.
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