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Endothelin ET A and ET B receptors mediate vascular smooth muscle contraction
Author(s) -
Sumner Michael J.,
Can Toby R.,
Mundin Jason W.,
White David G.,
Watts Ian S.
Publication year - 1992
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1992.tb14537.x
Subject(s) - contraction (grammar) , endothelin receptor , receptor , agonist , endothelin 1 , muscle contraction , vascular smooth muscle , endocrinology , medicine , chemistry , endothelins , stereochemistry , smooth muscle , biology
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 (EC 50 values ∼ 1 n m ), whereas, ET‐1 (EC 50 :4.5 n m ) was ∼ 80 fold more potent than ET‐3 in contracting RTA. In addition, the ET B receptor‐selective agonist [Ala 1,3,11,15 ]ET‐l contracted RJV (EC 50 :2.1 n m ) but not RTA. 3 The ET A receptor antagonist, BQ123, competitively antagonized (pA 2 6.93) the contraction of RTA produced by ET‐1, but had no effect (at 10 μ m ) on the contractile effects of either ET‐1, ET‐3 or [Ala 1,3,11,15 ]ET‐1 in RJV. 4 These data suggest that both ET A and ET B receptors can mediate vascular smooth muscle contraction.