Key result
ET(A) receptor activation by ET-1, but not ET-3 and S6b, is significantly modified by co-activation of ET(B) receptors, which decreases the potency of ET-1 in isolated rat mesenteric arteries.
Population
isolated rat mesenteric arteries
Design
Preclinical
Authors
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ET(B) co-activation may alter ET(A) antagonist affinity in vessels; leaves open translation to human endothelin pharmacology.
In rat mesenteric arteries, ET(B) receptor co-activation specifically modulates ET(A) receptor-mediated contractions induced by ET-1, altering its potency and antagonist affinity.
Adner et al. (2001) studied this question. Endothelin agonists (ET-1, S6b, ET-3, S6c) was evaluated on Arterial contraction. ET(A) receptor activation by ET-1, but not ET-3 and S6b, is significantly modified by co-activation of ET(B) receptors, which decreases the potency of ET-1 in isolated rat mesenteric arteries.
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