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. 1992 Nov;107(3):858-60.
doi: 10.1111/j.1476-5381.1992.tb14537.x.

Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction

M J Sumner  1 , T R Cannon, J W Mundin, D G White, I S Watts
Affiliations

Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction

M J Sumner et al. Br J Pharmacol. 1992 Nov.

Abstract

1. We have investigated the receptors mediating endothelin-induced contraction of rabbit isolated jugular vein (RJV) and rat isolated thoracic aorta (RTA). 2. Endothelin-1 (ET-1) and endothelin-3 (ET-3) contracted RJV preparations with similar potency (EC50 values approximately 1 nM), whereas, ET-1 (EC50:4.5 nM) was approximately 80 fold more potent than ET-3 in contracting RTA. In addition, the ETB receptor-selective agonist [Ala1,3,11,15]ET-1 contracted RJV (EC50:2.1 nM) but not RTA. 3. The ETA receptor antagonist, BQ123, competitively antagonized (pA2 6.93) the contraction of RTA produced by ET-1, but had no effect (at 10 microM) on the contractile effects of either ET-1, ET-3 or [Ala1,3,11,15]ET-1 in RJV. 4. These data suggest that both ETA and ETB receptors can mediate vascular smooth muscle contraction.

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