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血栓素受体可调节大鼠胃酸分泌。

Thromboxane receptors can modulate gastric acid secretion in the rat.

作者信息

Reeves J J, Stables R

机构信息

Department of Neuropharmacology, Glaxo Group Research Ltd., Herts, U.K.

出版信息

Prostaglandins. 1987 Dec;34(6):829-40. doi: 10.1016/0090-6980(87)90064-5.

Abstract

The effects of PGE2 and the thromboxane A2 mimetic, U-46619, have been investigated on gastric secretion in the rat isolated gastric mucosa. Both compounds produced concentration-related inhibitions of histamine-induced secretion whereas only U-46619 inhibited methacholine-stimulated and basal secretion, and neither compound had any effect on the secretory response to dbcAMP. Indomethacin had no effect on the antisecretory activity of PGE2 but markedly reduced the potency of U-46619 suggesting that endogenous prostaglandins play a role in the U-46619 responses. However, direct inhibitory effects of U-46619 were seen at high concentrations. The thromboxane receptor antagonist AH23848, at concentrations selective for thromboxane receptors, had no effect on responses to PGE2 but markedly inhibited the effects of U-46619. We conclude that the antisecretory profile of U-46619 differs from that of PGE2. U-46619 has both direct and indirect antisecretory effects and these are mediated via thromboxane receptors in the rat gastric mucosa.

摘要

已对前列腺素E2(PGE2)和血栓素A2类似物U - 46619对大鼠离体胃黏膜胃酸分泌的影响进行了研究。两种化合物均对组胺诱导的胃酸分泌产生浓度依赖性抑制,而只有U - 46619抑制乙酰甲胆碱刺激的胃酸分泌和基础胃酸分泌,且两种化合物对dbcAMP刺激的胃酸分泌反应均无影响。吲哚美辛对PGE2的抗分泌活性无影响,但显著降低了U - 46619的效力,提示内源性前列腺素在U - 46619的反应中起作用。然而,在高浓度时可观察到U - 46619的直接抑制作用。血栓素受体拮抗剂AH23848在对血栓素受体具有选择性的浓度下,对PGE2的反应无影响,但显著抑制U - 46619的作用。我们得出结论,U - 46619的抗分泌特征与PGE2不同。U - 46619具有直接和间接的抗分泌作用,且这些作用是通过大鼠胃黏膜中的血栓素受体介导的。

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