Haye-Legrand I, Bourdillat B, Labat C, Cerrina J, Norel X, Benveniste J, Brink C
INSERM U.200, Univ. Paris-Sud, Clamart.
Prostaglandins. 1987 Jun;33(6):845-54. doi: 10.1016/0090-6980(87)90113-4.
The effects of PGI2 and two analogs Iloprost and ZK 96480 were examined on isolated human pulmonary muscle preparations. High concentrations of these agents reduced the basal tone in all types of preparations. In addition, they relaxed tissues which had been maximally contracted with histamine (50 microM). PGI2 was more potent on pulmonary arterial muscle preparations (pD2 value: 6.33, n = 3) than on bronchial muscles. The relaxations induced by PGI2 in bronchial preparations were quite variable, that is, some tissues relaxed while others did not. The analogs also relaxed arterial preparations and the pD2 values were approximately the same (Iloprost: 7.42, n = 4 and ZK 96480: 7.48, n = 4). The isolated human pulmonary vascular preparations were approximately 10-fold more sensitive to the analogs than bronchial muscle preparations. In bronchial tissues we noted that the PGI2 relaxant effect was spontaneously reversed with time, an activity not observed with both analogs. A pretreatment of the bronchial tissues with indomethacin (1.7 microM) did not reduce the variations observed with PGI2 nor modify the transient relaxation observed with this agent. These data demonstrate that vascular tissues from the human lung are considerably more sensitive to these relaxant agonists than bronchial preparations.
研究了前列环素(PGI2)及其两种类似物伊洛前列素和ZK 96480对离体人肺肌标本的作用。这些药物的高浓度可降低所有类型标本的基础张力。此外,它们能使已用组胺(50微摩尔)最大程度收缩的组织松弛。PGI2对肺动脉肌标本(pD2值:6.33,n = 3)的作用比对支气管肌更强。PGI2在支气管标本中引起的松弛作用差异很大,即有些组织松弛而有些则不然。类似物也能使动脉标本松弛,且pD2值大致相同(伊洛前列素:7.42,n = 4;ZK 96480:7.48,n = 4)。离体人肺血管标本对类似物的敏感性比对支气管肌标本高约10倍。在支气管组织中,我们注意到PGI2的松弛作用会随时间自发逆转,而两种类似物均未观察到这种活性。用吲哚美辛(1.7微摩尔)预处理支气管组织既未减少PGI2观察到的变化,也未改变该药物引起的短暂松弛。这些数据表明,人肺的血管组织对这些松弛激动剂的敏感性远高于支气管标本。