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白三烯B4、C4和D4对豚鼠肺组织花生四烯酸代谢的刺激作用及体外血栓素A2的生成

Stimulation of arachidonic acid metabolism and generation of thromboxane A2 by leukotrienes B4, C4 and D4 in guinea-pig lung in vitro.

作者信息

Piper P J, Samhoun M N

出版信息

Br J Pharmacol. 1982 Oct;77(2):267-75. doi: 10.1111/j.1476-5381.1982.tb09295.x.

DOI:10.1111/j.1476-5381.1982.tb09295.x
PMID:6291685
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2044593/
Abstract

1 Leukotriene C4 (LTC4), LTD4, slow-reacting substance of anaphylaxis (SRS-A) (from guinea-pig lung), bradykinin (Bk) and arachidonic acid (AA) release thromboxane A2 (TxA2) and prostaglandin-like materials from guinea-pig isolated perfused lungs. 2 Release of TxA2 induced by LTC4 and LTD4 is inhibited by a thromboxane synthetase inhibitor, imidazole (2.9 mM). 3 Mepacrine (200 microM), a phospholipase inhibitor, inhibits release of TxA2 and prostaglandin-like materials caused by SRS-A and Bk but not that due to exogenous AA 4 Leukotrienes B4, C4 and D4 are approximately equipotent in inducing dose-related contractions of guinea-pig parenchymal strips (GPPs). 5 Leukotriene-induced contractions of GPPs are greatly inhibited by imidazole (2.9 mM), carboxyheptylimidazole (24 microM) and mepacrine (400 microM). 6 FPL 55712 (1.9 microM), the SRS-A antagonist, blocks contractions of GPPs induced by LTC4 and LTD4 but not those due to LTB4 or Bk. 7 Tachyphylaxis to LTB4 occurs in GPPs but not to LTC4 or LTD4. 8 These results suggest that in guinea-pig lung in vitro, LTB4, LTC4 and LTD4 activate a phospholipase with subsequent generation of cyclo-oxygenase products of which TxA2 plays an important role.

摘要

1 白三烯C4(LTC4)、白三烯D4(LTD4)、过敏反应慢反应物质(SRS - A,来自豚鼠肺)、缓激肽(Bk)和花生四烯酸(AA)可使豚鼠离体灌注肺释放血栓素A2(TxA2)和前列腺素样物质。2 血栓素合成酶抑制剂咪唑(2.9 mM)可抑制LTC4和LTD4诱导的TxA2释放。3 磷脂酶抑制剂米帕林(200 microM)可抑制SRS - A和Bk引起的TxA2和前列腺素样物质的释放,但不抑制外源性AA引起的释放。4 白三烯B4、C4和D4在诱导豚鼠实质条(GPPs)剂量相关的收缩方面大致等效。5 咪唑(2.9 mM)、羧基庚基咪唑(24 microM)和米帕林(400 microM)可显著抑制白三烯诱导的GPPs收缩。6 SRS - A拮抗剂FPL 55712(1.9 microM)可阻断LTC4和LTD4诱导的GPPs收缩,但不阻断LTB4或Bk引起的收缩。7 GPPs对LTB4会产生快速耐受性,但对LTC4或LTD4不会。8 这些结果表明,在体外豚鼠肺中,LTB4、LTC4和LTD4激活磷脂酶,随后生成环氧化酶产物,其中TxA2起重要作用。

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Stimulation of arachidonic acid metabolism and generation of thromboxane A2 by leukotrienes B4, C4 and D4 in guinea-pig lung in vitro.白三烯B4、C4和D4对豚鼠肺组织花生四烯酸代谢的刺激作用及体外血栓素A2的生成
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Leukotriene A: stereochemistry and enzymatic conversion to leukotriene B.白三烯A:立体化学及向白三烯B的酶促转化
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