October 1, 1986Journal of Medicinal ChemistryOpen Access

Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo

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Population

In vitro assays and in vivo model

Design

Preclinical

Follow-up

>3 hours postinfusion

Authors

STSuvit ThaisrivongsTulane University DPDonald T. PalsW.E. Upjohn Institute for Employment Research DHDouglas W. HarrisZoetis (United States)

Discussion

Member takes

Implication

Supports renin inhibitor development in primates; leaves open translation to human hypertension therapy.

Structured PICO

Population

In vitro assays (human plasma renin, porcine pepsin, bovine cathepsin D, rat liver homogenate) and in vivo model (furosemide-treated cynomolgus monkeys)

Intervention

Boc-Pro-Phe-N alpha-MeHis-Leu psi-[CHOHCH2]Val-Ile-Amp (XII) (5 mg/kg iv in vivo)

Outcome

Inhibition of plasma renin activity and blood pressure loweringsurrogate

The novel renin inhibitor XII demonstrates potent, specific in vitro activity and prolonged in vivo hypotensive effects in a primate model.

Cite This Study

Thaisrivongs et al. (1986) studied this question.

synapsesocial.com/papers/6a8acba4de5ec4e001e3a32b https://doi.org/10.1021/jm00160a049

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Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Also Consider