Reimer R, Heim H K, Muallem R, Odes H S, Sewing K F
Institute of Pharmacology, Medical School, Hanover, FRG.
Prostaglandins. 1992 Nov;44(5):485-93. doi: 10.1016/0090-6980(92)90142-g.
Rank order of agonist potency for activation of adenylate cyclase by the naturally occurring prostanoids PGE2, PGF2 alpha, PGD2, the stable PGI2 analogue iloprost, and the TXA2 mimetic U 46619, provides evidence for the existence of a distinct PGE-receptor on guinea-pig duodenal enterocytes. The PGE-receptor is likely to be of the EP2-subtype since the specific EP2-agonist 11-deoxy-PGE1 stimulated adenylate cyclase activity with a 20-fold higher potency than the EP1-agonist 17-phenyltrinor-PGE2 and the EP3-agonists MB 28767 and GR 63799. In addition, sulprostone (acting on both EP1- and EP3-receptors) was ineffective. Since the specific EP1-antagonist SC 19220 did not inhibit PGE2-stimulated adenylate cyclase activity, the involvement of EP1-receptors could be further excluded. The synthetic prostaglandin E-analogues misoprostol and nocloprost stimulated adenylate cyclase almost identically, though they were about 10-fold less potent than the natural PGE2.
天然存在的前列腺素PGE2、PGF2α、PGD2、稳定的前列环素类似物伊洛前列素以及血栓素A2模拟物U 46619激活腺苷酸环化酶的激动剂效力的排名顺序，为豚鼠十二指肠肠细胞上存在独特的PGE受体提供了证据。PGE受体可能是EP2亚型，因为特异性EP2激动剂11-脱氧-PGE1刺激腺苷酸环化酶活性的效力比EP1激动剂17-苯基三降-PGE2以及EP3激动剂MB 28767和GR 63799高20倍。此外，舒前列素（作用于EP1和EP3受体）无效。由于特异性EP1拮抗剂SC 19220不抑制PGE2刺激的腺苷酸环化酶活性，因此可以进一步排除EP1受体的参与。合成前列腺素E类似物米索前列醇和诺克洛前列醇刺激腺苷酸环化酶的作用几乎相同，尽管它们的效力比天然PGE2低约10倍。
