Armstrong J M, Boura A L, Hamberg M, Samuelsson B
Eur J Pharmacol. 1976 Oct;39(2):251-8. doi: 10.1016/0014-2999(76)90133-3.
The vasodepressor actions of the cyclic endoperoxides PGG2 and PGH2 were compared with those of their products PGD2 and PGE2 using anaesthetised normotensive and genetically hypertensive rats. Given into the aortic arch of normotensives PGE2 was approximately 6 times more potent than PGH2 and 11 times more potent than PGG2 and PGD2. Hypertensive animals were 1.5-10 times more sensitive than normotensives to the depressor effects of PGG2 and PGH2, but their sensitivity to either PGD2 or PGE2 was similar. Thus in hypertensives the endoperoxides may be converted more readily to PGE2 and other products. In both types of rat PGG2 and PGH2 given intravenously were as active or more active than after intra-arterial. Therefore PGG2 and PGH2 may be converted more readily to more active products during passage through the lungs but whereas small doses of PGE2 are almost completely eliminated large doses may saturate uplmonary removal mechanisms.
利用麻醉的正常血压大鼠和遗传性高血压大鼠,比较了环内过氧化物PGG2和PGH2与其产物PGD2和PGE2的血管降压作用。将PGE2注入正常血压大鼠的主动脉弓,其效力约为PGH2的6倍,PGG2和PGD2的11倍。高血压动物对PGG2和PGH2降压作用的敏感性比正常血压动物高1.5至10倍,但它们对PGD2或PGE2的敏感性相似。因此,在高血压动物中,内过氧化物可能更容易转化为PGE2和其他产物。在两种类型的大鼠中,静脉注射PGG2和PGH2的活性与动脉内注射后的活性相同或更高。因此,PGG2和PGH2在通过肺部时可能更容易转化为活性更高的产物,但小剂量的PGE2几乎完全被清除,而大剂量可能会使肺部清除机制饱和。