January 1, 2013Biological and Pharmaceutical BulletinOpen Access

Pharmacological Characterization of BR-A-657, a Highly Potent Nonpeptide Angiotensin II Receptor Antagonist

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Population

In vitro models and in vivo models.

Comparison

BR-A-657 vs Vehicle control and active comparators

Design

Preclinical

Follow-up

up to 24 hours

Authors

YHYong HaSunchon National University JLJoo Han LeeBoryung Pharma (South Korea)JKJe Hak KimBoryung Pharma (South Korea)

Discussion

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Implication

Supports preclinical development of BR-A-657; leaves open translation to human efficacy and safety.

Structured PICO

Population

In vitro models (HEK-293 cells, isolated rabbit thoracic aorta) and in vivo models (conscious normotensive Sprague-Dawley rats, furosemide-treated rats, and renal hypertensive rats).

Intervention

BR-A-657 (intravenous 0.01-10 mg/kg or oral 1-3 mg/kg)

Comparator

Vehicle control and active comparators (losartan, valsartan)

Outcome

AT1 receptor binding affinity (IC50), inhibition of Ang II-induced contraction, and reduction in mean arterial pressuresurrogate

BR-A-657 is a highly potent, nonpeptide AT1 receptor antagonist that effectively lowers blood pressure in hypertensive rat models, suggesting potential as a novel antihypertensive agent.

Cite This Study

Ha et al. (2013) studied this question.

synapsesocial.com/papers/6a7cf6f99092f18ef00eb4f0 https://doi.org/10.1248/bpb.b12-00966

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Pharmacological Characterization of BR-A-657, a Highly Potent Nonpeptide Angiotensin II Receptor Antagonist

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Pharmacological Characterization of BR-A-657, a Highly Potent Nonpeptide Angiotensin II Receptor Antagonist

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Also Consider