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食蟹猴中血栓素B2的代谢

Metabolism of thromboxane B2 in the cynomolgus monkey.

作者信息

Kindahl H

出版信息

Prostaglandins. 1977 Apr;13(4):619-29. doi: 10.1016/0090-6980(77)90233-7.

Abstract

[5,6,8,9,11,12,14,15-3H8]-Thromboxane B2 was injected into the saphenous vein of female cynomolgus monkeys, and blood samples were withdrawn from the contralateral saphenous vein. The compound was eliminated from the circulation with a half-life of about 10 min after an initial rapid disappearance. Some more polar products appeared with time, and also small amounts of material less polar than thromboxane B2; however, the dominating compound in all blood samples was unconverted thromboxane B2. About 45% of the given dose of tritium was excreted into urine in 48 hrs. Several metabolites of thromboxane B2 were found. The major urinary metabolite was identified as dinorthromboxane B2 (about 32% of urinary radioactivity). Unconverted thromboxane B2 was also found in considerable amounts (13% of urinary radioactivity). It is concluded that 1) dehydrogenation at C-12 is not a major pathway in the degradation of this compound, in contrast to metabolism at the corresponding C-15 alcohol group of prostaglandins; 2) after having gained access to the circulation, thromboxane B2 is the main circulating compound; however, assay of thromboxane B2 in plasma will be complicated or precluded by large artifactual production of the compound by platelets during sample collection.

摘要

将[5,6,8,9,11,12,14,15 - 3H8] - 血栓素B2注入雌性食蟹猴的隐静脉,然后从对侧隐静脉采集血样。该化合物在最初快速消失后,以约10分钟的半衰期从循环中消除。随着时间推移出现了一些极性更强的产物,还有少量极性比血栓素B2弱的物质;然而,所有血样中的主要化合物是未转化的血栓素B2。给予剂量中约45%的氚在48小时内随尿液排出。发现了血栓素B2的几种代谢产物。主要的尿代谢产物被鉴定为双去甲血栓素B2(约占尿放射性的32%)。也发现了相当数量的未转化血栓素B2(占尿放射性的13%)。得出以下结论:1)与前列腺素相应的C - 15醇基的代谢不同,C - 12位的脱氢不是该化合物降解的主要途径;2)进入循环后,血栓素B2是主要的循环化合物;然而,在样本采集过程中血小板会大量人为产生该化合物,这会使血浆中血栓素B2的测定变得复杂或无法进行。

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