EFFECTS OF EP-RECEPTOR SUBTYPE SPECIFIC AGONISTS AND OTHER PROSTANOIDS ON ADENYLATE-CYCLASE ACTIVITY OF DUODENAL EPITHELIAL-CELLS
EFFECTS OF EP-RECEPTOR SUBTYPE SPECIFIC AGONISTS AND OTHER PROSTANOIDS ON ADENYLATE-CYCLASE ACTIVITY OF DUODENAL EPITHELIAL-CELLS
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DOI：
10.1016/0090-6980(92)90142-g
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发表时间：
1992-11-01
期刊：
影响因子：
--
通讯作者：
SEWING, KF
中科院分区：
文献类型：
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作者：
REIMER, R;HEIM, HK;SEWING, KF
天然存在的前列腺素PGE2、PGF2alpha、PGD2、稳定的PGI2类似物iloprost和TXA2模拟物u46619对腺苷酸环化酶激活的激动剂效价排序，为豚鼠十二指肠肠细胞上存在独特的pge受体提供了证据。这种pge受体可能属于ep2亚型，因为特异性的ep2激动剂11-脱氧- pge能刺激腺苷酸环化酶活性，其效力比ep1激动剂17-苯三基- pge2和ep3激动剂MB 28767和GR 63799高20倍。此外，磺胺酮（同时作用于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。合成的前列腺素e类似物米索前列醇和诺氯前列素对腺苷酸环化酶的刺激几乎相同，尽管它们的效力比天然的PGE2低10倍左右。
Rank order of agonist potency for activation of adenylate cyclase by the naturally occurring prostanoids PGE2, PGF2alpha, 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. This PGE-receptor is likely to be of the EP2-Subtype since the specific EP2-agonist 11-deoxy-PGE, 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.