作者: S. Uhlig , Roland Lewis Featherstone
DOI: 10.1007/PL00005067
关键词:
摘要: To gain more insight into the complex pulmonary interactions of endothelins (ET), we studied airway and vascular responses to in isolated perfused rat lungs presence novel ETB-receptor antagonist BQ788. In particular focused on prostacyclin release. The effectiveness BQ788 our system was shown by its ability concentration-dependently prevent vasoconstriction (IC50 0.1μM), bronchoconstriction 0.1μM) production (IC50<0.1μM) induced agonist IRL1620 (1nmol). Airway ET-1: ET-1-induced aggravated BQ123 (1 or 8μM), while pretreatment 8μM) showed no significant effect. Simultaneous treatment with 8μM attenuated bronchoconstriction. Vascular ET-1 (1nmol)-induced potentiated but ETA-receptor (1μM). diminished amounts stable metabolite 6-keto-PGF1α were detected perfusate. completely prevented vasoconstriction. Conclusions: Both ETA- ETB-receptors contribute is stimulation ETB-receptors, a response that partly mediated prostacyclin. Due mutual between simultaneous inhibition both receptors required deleterious effects lung functions.