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ANGIOTENSIN RECEPTORS IN BOVINE UMBILICAL ARTERY AND THEIR INHIBITION BY NONSTEROIDAL ANTI‐INFLAMMATORY DRUGS
Author(s) -
GOODFRIEND THEODORE L.,
SIMPSON ROBERT U.
Publication year - 1981
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.1476-5381.1981.tb09121.x
Subject(s) - angiotensin ii , chemistry , contraction (grammar) , pharmacology , receptor , angiotensin receptor , renin–angiotensin system , umbilical artery , medicine , phenylbutazone , endocrinology , biochemistry , biology , blood pressure , pregnancy , fetus , genetics
1 The contractile effect of angiotensin II on bovine isolated umbilical arteries was compared to [ 125 I]‐angiotensin II binding by a subcellular fraction of that tissue. The ED 50 of angiotensin was 3.1 ± 2.8 × 10 −8 m , while the apparent dissociation constant was 4.9 ± 1.6 × 10 −9 m . 2 Indomethacin, meclofenamate, and eicosatetraynoic acid inhibited angiotensin‐induced contraction of the isolated artery and binding to a particulate fraction at comparable doses. Phenylbutazone inhibited [ 125 I]‐angiotensin binding more potently than the response. Inhibition by the first three agents was noncompetitive, whereas phenylbutazone inhibited competitively. 3 Inhibition of angiotensin activity by the nonsteroidal anti‐inflammatory agents was not specific. These agents also inhibited 5‐hydroxytryptamine‐induced contraction, but not the contraction induced by KCl. 4 The data suggest that the angiotensin binding sites studied include receptors that mediate contraction of the isolated umbilical artery. Our data also indicate that indomethacin, meclofenamate, eicosatetraynoic acid and phenylbutazone are capable of direct inhibitory effects on receptors, as well as their well‐known synthetase actions. The net effect of these activities will determine the change these agents cause in tissue responses to hormones.