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用于研究心脏和肝脏区域代谢的长链F-18脂肪酸;小鼠代谢的奇偶效应。

Long-chain F-18 fatty acids for the study of regional metabolism in heart and liver; odd-even effects of metabolism in mice.

作者信息

Knust E J, Kupfernagel C, Stöcklin G

出版信息

J Nucl Med. 1979 Nov;20(11):1170-5.

PMID:317095
Abstract

In view of the potential usefulness of fluorine-tagged fatty acids in the study of regional metabolism in the heart and liver, the time courses of uptake and release of 9,10-[18F]fluorostearic acid, 2-[18F]fluorostearic acid, 16-[18F]fluorohexadecanoic acid, 17-[18F]fluoroheptadecanoic acid have been investigated in several organs of NMRI mice. Whereas 2-[18F]fluorostearic acid shows very little uptake in the heart muscle but an increasing accumulation in the liver, the fatty acids with the F-18 label in the middle or at the end of the carbon chain exhibit uptake and elimination behavior similar to that of the analogous C-11-labeled compounds. After rapid concentration in the heart within 1 min, clearance takes place with fast and slow components. 16-[18F]fluorohexadecanoic acid and 17-[18F]fluoroheptadecanoic acid have different half-times of elimination. These differences are also reflected by the fact that nearly all the activity present in the heart can be recovered as fluoride(F-18) in the case of 17-[18F]fluoroheptadecanoic acid, whereas practically no fluoride was found among the metabolites of 16-[18F]fluorohexadecanoic acid. Similar differences were observed for the F-18 activity in bone. The results can be interpreted in terms of the odd-even rule: beta oxidation of even-numbered fatty acids ends up with [18F]fluoroacetic acid, whereas the odd-numbered fatty acids give rise to beta-[18F]fluoropropionic acid. Only in the latter case does dehalogenation take place leading to free fluoride, whereas fluoroacetic acid undergoes further reactions in the citric acid cycle.

摘要

鉴于氟标记脂肪酸在心脏和肝脏区域代谢研究中的潜在用途,已在NMRI小鼠的多个器官中研究了9,10-[¹⁸F]氟硬脂酸、2-[¹⁸F]氟硬脂酸、16-[¹⁸F]氟十六烷酸、17-[¹⁸F]氟十七烷酸的摄取和释放时间过程。2-[¹⁸F]氟硬脂酸在心肌中的摄取很少,但在肝脏中的积累却在增加,而碳链中间或末端带有F-18标记的脂肪酸表现出与类似的C-11标记化合物相似的摄取和消除行为。在1分钟内快速在心脏中浓缩后,清除过程有快、慢两个成分。16-[¹⁸F]氟十六烷酸和17-[¹⁸F]氟十七烷酸具有不同的消除半衰期。这些差异还体现在以下事实上:对于17-[¹⁸F]氟十七烷酸,心脏中几乎所有的放射性都可以作为氟化物(F-18)回收,而在16-[¹⁸F]氟十六烷酸的代谢产物中几乎没有发现氟化物。在骨骼中的F-18活性也观察到类似差异。结果可以根据奇偶规则来解释:偶数脂肪酸的β氧化最终产生[¹⁸F]氟乙酸,而奇数脂肪酸则产生β-[¹⁸F]氟丙酸。只有在后一种情况下才会发生脱卤反应生成游离氟化物,而氟乙酸会在柠檬酸循环中发生进一步反应。

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