Polakowski J S, Opgenorth T J, Pollock D M
Abbott Laboratories, Abbott Park, Illinois 60064, USA.
Biochem Biophys Res Commun. 1996 Aug 5;225(1):225-31. doi: 10.1006/bbrc.1996.1158.
The effect of ETA receptor blockade on the bronchopulmonary response to endothelin-1 was determined in the airway of the anesthetized, spontaneously breathing guinea pig. Endothelin-1 administered as an aerosol increased lung resistance and decreased dynamic lung compliance. Delivery of the ETA receptor antagonist, FR139317, 5 min prior to giving endothelin-1 greatly potentiated these changes. A lower dose of endothelin-1 that had no effect on resistance or compliance produced large and significant changes when pretreated with FR139317. In contrast, aerosolized FR139317 had no effect on the bronchopulmonary response to intravenously administered endothelin-1. These data suggest a non-contractile function of ETA receptors accessible from the airways that serve to buffer the constrictor effects of non-ETA receptors.
在麻醉状态下自主呼吸的豚鼠气道中，测定了内皮素A（ETA）受体阻断对支气管肺对内皮素-1反应的影响。雾化给予内皮素-1会增加肺阻力并降低动态肺顺应性。在给予内皮素-1前5分钟给予ETA受体拮抗剂FR139317，会极大地增强这些变化。预先用FR139317处理时，较低剂量的内皮素-1对阻力或顺应性无影响，但会产生显著的大变化。相比之下，雾化的FR139317对静脉注射内皮素-1引起的支气管肺反应无影响。这些数据表明，气道中可及的ETA受体具有非收缩功能，可缓冲非ETA受体的收缩作用。
