Dajani E Z, Driskill D R
Prostaglandins. 1977 Oct;14(4):659-65. doi: 10.1016/0090-6980(77)90193-9.
The compound 7-OPyA has been reported to antagonize smooth muscle stimulatory effects of some prostaglandins (PG's) in vitro. The in vivo PG antagonist activity of 7-OPyA has not been adequately diarrhea in mice. We studied the effects of this compound on PGE1. Secretion was stimulated by continuous intravenous infusion of histamine. At the steady-state plateau of gastric secretion, PGE1 methyl ester (PGE1 ME) or PGE1 ME and 7-OPyA were simultaneously infused intravenously. The extent of gastric secretory inhibition afforded by PGE1 ME alone or in the presence of 7-OPyA was assessed. 7-OPyA did not modify PGE1 ME gastric antisecretory actions when administered at doses 20-50 times greater than the dose of PGE1 ME. These results suggest that the prostaglandin antagonist effects of 7-OPyA show organ specificity, which may be of clinical importance.
据报道,化合物7-OPyA在体外可拮抗某些前列腺素(PG)对平滑肌的刺激作用。7-OPyA在体内的PG拮抗剂活性在小鼠腹泻方面尚未得到充分研究。我们研究了该化合物对PGE1的影响。通过持续静脉输注组胺刺激分泌。在胃酸分泌的稳态平台期,静脉同时输注PGE1甲酯(PGE1 ME)或PGE1 ME与7-OPyA。评估单独使用PGE1 ME或在7-OPyA存在下胃酸分泌抑制的程度。当以比PGE1 ME剂量大20至50倍的剂量给药时,7-OPyA不会改变PGE1 ME的胃酸分泌抑制作用。这些结果表明,7-OPyA的前列腺素拮抗剂作用具有器官特异性,这可能具有临床重要性。