Effect of different endothelin receptor antagonists and of the novel non‐peptide antagonist Ro 46‐2005 on endothelin levels in rat plasma
Why the study?
Does Ro 46-2005 alter plasma concentrations of ET-1, big ET-1, and ET-3 compared to selective ETA antagonists in conscious rats?
Population
Conscious rats
Comparison
Ro 46-2005, a non-peptide antagonist of ETA and… vs Selective peptide ETA antagonists BQ-123 and…
Design
Preclinical
Follow-up
15 min (peak effect)
Authors
Discussion
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Implication
Combined ETA/ETB antagonism elevates ET-1 unlike selective ETA blockade in rats; leaves open receptor-specific clearance mechanisms for human translation.
Structured PICO
Does Ro 46-2005 alter plasma concentrations of ET-1, big ET-1, and ET-3 compared to selective ETA antagonists in conscious rats?
P
Population
Conscious rats
I
Intervention
Ro 46-2005 (10 mg/kg, i.v.), a non-peptide antagonist of ETA and ETB receptors
C
Comparator
Selective peptide ETA antagonists BQ-123 and FR-139317, and basal levels
O
Outcome
Plasma concentrations of ET-1, big ET-1, and ET-3surrogate
The combined ETA/ETB receptor antagonist Ro 46-2005 increases plasma ET-1 levels in rats, likely due to displacement from ETB receptors, an effect not seen with selective ETA antagonists.
Cite This Study
Löffler et al. (1993) studied this question.