Endothelin-1 enhances vascular permeability in the rat heart through the ETA receptor.
Intravenous injection of endothelin-1 (ET-1, 0.1 and 1 nmol/kg) resulted in a dose-dependent increase in vascular permeability in the coronary circulation of conscious rats. The increase was almost completely abolished by the selective ETA receptor antagonist, BQ-123 (1 mg/kg). The ET-1 analogue, [Trp(For)21]ET-1, which is devoid of the depressor but not the pressor activity, evoked changes in protein extravasation similar to those with ET-1. These data indicate that the permeability effect of ET-1 is mediated through the ETA receptor.
Filep
J G
JG
Department of Pharmacology, Faculty of Medicine, University of Sherbrooke, P.Q., Canada.
Földes-Filep
E
E
Rousseau
A
A
Fournier
A
A
Sirois
P
P
Yano
M
M
D000818:Animals; D002199:Capillary Permeability / Q000187:drug effects*; D003331:Coronary Vessels / Q000187:drug effects*; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000494:pharmacology*; D008297:Male; D010456:Peptides, Cyclic / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D017466:Receptors, Endothelin / Q000378:metabolism*
D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D010456:Peptides, Cyclic; D017466:Receptors, Endothelin; C072247:cyclo(Trp-Asp-Pro-Val-Leu)