Key result
Dual ETA/ETB antagonism is required to block endothelin-mediated vasoconstriction in human vessels.
Why the study?
The roles of ETA and ETB receptors in mediating endothelin-1 induced contraction in human blood vessels were not fully characterized.
Inhibition of endothelin-induced contraction in patients requires the use of combined ETA/ETB antagonists because both receptors mediate contraction in human blood vessels.
Answers are grounded in this paper and cite their sources.
Combined ETA/ETB antagonism may be needed to blunt endothelin-1 contraction; leaves open clinical utility of dual blockade.
Vascular smooth muscle cells of human IMA, IMV, and PCA contain both ETA and ETB receptors, whereas the endothelium of IMA and PCA does not express functional ETB receptors linked to nitric oxide and/or prostacyclin production. Hence, inhibition of endothelin-induced contraction in patients requires the use of combined ETA/ETB antagonists.
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Seo et al. (1994) studied this question. Combined ETA/ETB antagonists are required to inhibit endothelin-induced contraction in patients because both ETA and ETB receptors mediate contraction in human blood vessels.
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