Circulation, Vol 89, 1203-1208, Copyright © 1994 by American Heart Association
B Seo, BS Oemar, R Siebenmann, L von Segesser and TF Luscher
BACKGROUND: Endothelin (ET)-1 has potent vascular effects. Two endothelin
receptors have been cloned, namely, the ETA receptor, which preferentially
binds ET-1, and the ETB receptor, which equally binds ET- 1 and ET-3 and
preferentially sarafotoxin S6c. We characterized endothelin receptor
subtypes on vascular smooth muscle and endothelium of isolated human
internal mammary artery (IMA) and vein (IMV) and porcine coronary artery
(PCA) using the ETA antagonists FR139317 and BQ- 123, the ETB ligand
sarafotoxin S6c, and the ETA/ETB antagonist Ro 47- 0203 (bosentan). METHODS
AND RESULTS: In endothelium-denuded IMA and PCA and less so in IMV,
FR139317 and BQ-123 (in PCA only) shifted the concentration-contraction
curves to ET-1 parallel to the right. However, even at 10(-5) mol/L,
FR139317 did not inhibit a high- sensitivity portion of the
concentration-contraction curve. Moreover, the ETB receptor agonist
sarafotoxin S6c induced contraction in vessels preincubated with FR139317.
IMV was significantly more sensitive to the contractile effect of ET-1 and
sarafotoxin S6c than was IMA (P < .05). Prolonged incubation with
sarafotoxin S6c (to downregulate ETB receptors) and FR139317 eliminated the
contraction resistant to FR139317. The ETA/ETB receptor antagonist bosentan
caused a parallel shift of the concentration-contraction curve to the right
at all concentrations of endothelin. ETB receptor mRNA was detected by
Northern blot analysis in IMA and aortic smooth muscle cells. In
precontracted IMA and PCA with endothelium, sarafotoxin S6c did not cause
endothelium-dependent relaxations, whereas transient responses occurred in
IMV. CONCLUSIONS: 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.
ARTICLES
Both ETA and ETB receptors mediate contraction to endothelin-1 in human blood vessels
Department of Research, University Hospitals, Basel, Switzerland.
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