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June 1, 1995Hypertension

Antihypertensive Effects of a Novel Endothelin-A Receptor Antagonist in Rats

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Why the study?

Does the endothelin-A receptor antagonist BMS-182874 reduce blood pressure in rat models of hypertension?

Population

Sprague-Dawley rats, conscious deoxycorticosterone acetate-salt hypertensive rats, spontaneously…

Design

Preclinical

Follow-up

3 days

Authors

JBJ. Eileen BirdBristol-Myers Squibb (Germany)SMSuzanne MorelandBristol-Myers Squibb (United States)TWThomas L. WaldronHôpital Raymond-Poincaré

Discussion

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Implication

Endothelin-A antagonism shows model-specific BP effects in rats; leaves open relevance to human hypertension subtypes.

Structured PICO

Does the endothelin-A receptor antagonist BMS-182874 reduce blood pressure in rat models of hypertension?

P
Population
Sprague-Dawley rats, conscious deoxycorticosterone acetate (DOCA)-salt hypertensive rats, spontaneously hypertensive rats (SHR), and sodium-deplete SHR
I
Intervention
BMS-182874 (endothelin-A receptor antagonist) administered intravenously (30, 100, or 300 mumol/kg) or orally (75, 150, or 450 mumol/kg) for up to 3 days
O
Outcome
Changes in mean arterial pressure / blood pressuresurrogate

BMS-182874 is an orally active endothelin-A receptor antagonist that effectively lowers blood pressure in mineralocorticoid hypertension models but has less effect in sodium-replete and sodium-deplete spontaneously hypertensive rats.

Cite This Study

Bird et al. (1995) studied this question.

synapsesocial.com/papers/6a86b03f740e6cf4b5cf7b03https://doi.org/10.1161/01.hyp.25.6.1191

Topics

Hypertension management
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1The Discovery of Sulfonamide Endothelin Antagonists and the Development of the Orally Active ETA Antagonist 5-(Dimethylamino)-N-(3,4-dimethyl-5- isoxazolyl)-1-naphthalenesulfonamide1994 · 137 citations
  2. 2Effects of WAY-123,398, a New Class III Antiarrhythmic Agent, on Cardiac Refractoriness and Ventricular Fibrillation Threshold in Anesthetized Dogs: A Comparison with UK-68798, E-4031, and dl-Sotalol1992 · 62 citations
  3. 3Potential role of endothelin in hypertension. Controversy on endothelin in hypertension.1993 · 134 citations
  4. 4Is endothelin involved in the pathogenesis of hypertension?1993 · 103 citations
  5. 5Effect of Phosphoramidon (Endothelin Converting Enzyme Inhibitor) and BQ-123 (Endothelin Receptor Subtype A Antagonist) on Blood Pressure in Hypertensive Rats1993 · 46 citations