Key result
Nonpeptidic ETA- and ETB-receptor antagonists (BMS-182874 and A-192621) reversed ET-1-induced sustained increases of cytosolic and nuclear calcium in human aortic vascular smooth muscle cells.
Population
human aortic vascular smooth muscle cells (hVSMCs)
Comparison
Nonpeptidic antagonists of ETA (BMS-182874… vs Peptidic antagonists of ETA (BQ-123, 10 mol/L)…
Design
Preclinical
Authors
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May position nonpeptidic ET antagonists as superior research tools for vascular calcium signaling; leaves open clinical translation.
Nonpeptidic ETA- and ETB-receptor antagonists can reverse ET-1-induced sustained intracellular calcium increases in human aortic vascular smooth muscle cells, unlike peptidic antagonists, suggesting they may be superior pharmacological tools for this purpose.
Bkaily et al. (2008) studied this question. Nonpeptidic antagonists of ETA and ETB receptors (BMS-182874 and A-192621) vs. Peptidic antagonists (BQ-123 and BQ-788) was evaluated on Reversal of ET-1-induced sustained increase of cytosolic and nuclear calcium. Nonpeptidic ETA- and ETB-receptor antagonists (BMS-182874 and A-192621) reversed ET-1-induced sustained increases of cytosolic and nuclear calcium in human aortic vascular smooth muscle cells.
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