Key result
Oral renin inhibitor compound 8i lowers blood pressure for ~2 hours in marmosets.
Why the study?
Development of potent and specific human renin inhibitors with effective blood pressure lowering activity was needed to advance therapeutic options targeting the renin-angiotensin system.
Does the renin inhibitor compound 8i inhibit human renin and lower blood pressure in salt-depleted marmosets?
Population
In vitro human renin, pepsin, and cathepsin D assays and salt-depleted marmosets
Comparison
Renin inhibitor compound 8i versus related aspartic proteinases and baseline
Design
Preclinical synthesis and biological activity study
Follow-up
Up to 2 hours after oral administration
Authors
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Shortened renin inhibitor 8i extends SAR for transition-state mimics; leaves open in vivo efficacy and clinical translation.
Does the renin inhibitor compound 8i inhibit human renin and lower blood pressure in salt-depleted marmosets?
Compound 8i is a highly specific, orally active transition-state inhibitor of human renin that lowers blood pressure in a preclinical model.
Fuhrer et al. (1988) studied this question. Compound 8i was evaluated on IC50 against human renin and blood pressure reduction. Compound 8i demonstrated an IC50 of 2 x 10(-9) M against human renin and lowered blood pressure for up to 2 hours after a 10 mg/kg oral dose in salt-depleted marmosets.
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