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应用１９Ｆ体内核磁共振技术（１９ＦＮＭＲ）直接观测了５－氟尿嘧啶（５－ＦＵ）在小鼠肝脏中的代谢产物和代谢动力学，昆明种（ＫＭ）小鼠和Ｃ５７小鼠ｉｖ５－ＦＵ２００ｍｇ·ｋｇ－１后，用１９Ｆ表面线圈测得５－ＦＵ在肝脏中依次代谢为α－氟－β－脲基丙酸（ＦＵＰＡ）和α－氟－β－丙氨酸（ＦＢＡＬ）．在荷Ｓ１８０瘤ＫＭ小鼠肝脏中还可检测到活化产物氟代核苷／核苷酸（ＦＮＵＣ）．５－ＦＵ在ＫＭ和Ｃ５７小鼠肝脏中清除较快，消除半衰期分别为１６．７±３．０和３６．６±２．４ｍｉｎ，其主要产物ＦＢＡＬ的最大生成ｒｍａｘ（相对强度比）分别为８４±１４和９２±１０．但在ＫＭ小鼠肝脏中由ＦＵＰＡ进一步降解为ＦＢＡＬ的速率明显快于Ｃ５７小鼠，ｔ１／２ｒ分别为３１±８和５７±１３ｍｉｎ．相应地，在Ｃ５７小鼠肝脏中ＦＵＰＡ能维持一定的水平并达到ｒｍａｘ２６．２±２．２．
The metabolites and the pharmacokinetics of 5-fluorouracil (5-FU) in mouse liver were directly observed by 19F in vivo magnetic resonance imaging (19F NMR), Kunming (KM) mice and C57 mice iv5-FU at 200 mg · kg- 1, 5-FU was sequentially metabolized in the liver to α-fluoro- β-ureido propionic acid (FUPA) and α-fluoro-β-alanine (FBAL) as measured by 19F surface coils. The activation product, Fluoromonosine / Nucleotide (FNUC), was also detectable in the livers of S180-bearing KM mice. 5-FU was rapidly cleared in the liver of KM and C57 mice with elimination half-lives of 16.7 ± 3.0 and 36.6 ± 2.4 min, respectively. The maximum product of maximal product rmax (relative intensity ratio) of 5-FU was 84 ± 14 and 92 ± 10. However, the rate of further degradation of FALA to FBAL by FUPA in the liver of KM mice was significantly faster than that of C57 mice with t1 / 2r of 31 ± 8 and 57 ± 13 min, respectively. Accordingly, FUPA was maintained at a level of rmax26.2 ± 2.2 in C57 mouse livers.