Disposition of radioactivity after injection of liver-targeted proteins labeled with 111In or 125I. Effect of labeling on distribution and excretion of radioactivity in rats.
Disposition of radioactivity after injection of liver-targeted proteins labeled with 111In or 125I. Effect of labeling on distribution and excretion of radioactivity in rats.
复制标题
注射用 111In 或 125I 标记的肝脏靶向蛋白后放射性的处置。
DOI：
10.1021/js9804415
复制
发表时间：
1999
影响因子：
3.8
通讯作者：
M. Hashida
中科院分区：
文献类型：
--
作者：
F. Staud;M. Nishikawa;K. Morimoto;Y. Takakura;M. Hashida
研究了放射性标记肝脏特异性蛋白对体内放射性处置的影响。研究了111In和125I作为放射性标记在体内蛋白质配置研究中的适用性。半乳糖化和阳离子化的牛血清白蛋白分别用125I（氯胺- t法）或111In标记，用1-（4-异硫氰酸苄基）乙二胺四乙酸（SCN-BZ-EDTA）或二乙烯三胺五乙酸（DTPA）作为双功能螯合剂（bca）静脉注射给大鼠。125I放射性迅速从肝脏消失，随后随尿液和胆汁排出，主要以TCA可溶性部分排出。111另一方面，在实验期间，与碘相关的放射性在肝组织中保持了相当高的量，并且与125I相比，在胆汁和尿液中排泄的程度较低。当比较BCA对111In放射性排泄的影响时，在尿清除率方面没有观察到显著差异。然而，胆道排泄的111in - scn - bz - edta结合放射性显著升高。总之，与125I相比，111In标记似乎更准确地表征了大鼠静脉给药后肝脏靶向蛋白的体内分布，并允许进行更准确的药代动力学评估。
The effect of radiolabeling liver-specific proteins on the in vivo disposition of radioactivity was investigated. The suitability of 111In and 125I as radiolabels for protein disposition studies in vivo was examined. Galactosylated and cationized bovine serum albumin were labeled with either 125I by the chloramine-T method or 111In, using 1-(4-isothiocyanatobenzyl)ethylenediaminetetraacetic acid (SCN-BZ-EDTA) or diethylenetriaminepentaacetic acid (DTPA) as bifunctional chelating agents (BCAs) and administered intravenously to rats. 125I radioactivity disappeared rapidly from the liver with subsequent excretion in the urine and bile, mainly in the TCA soluble fraction. 111In-associated radioactivity, on the other hand, remained in the hepatic tissue in considerably higher amounts during the experiment and was excreted in the bile and urine to a lower extent when compared with 125I. When the effect of BCA on excretion of 111In radioactivity was compared, no significant differences were observed in the urinary clearances. However, biliary excretion was significantly higher for 111In-SCN-BZ-EDTA-bound radioactivity. In conclusion, when compared with 125I, 111In labeling seems to more accurately characterize the in vivo distribution of liver-targeted proteins after their iv administration in rats and allows a more accurate pharmacokinetic evaluation to be performed.
登录
查看更多内容
影响因子：
11.2
作者：
F. Geissler;S. K. Anderson;P. Venkatesan;O. Press
通讯作者：
F. Geissler;S. K. Anderson;P. Venkatesan;O. Press
DOI：
--
发表时间：
1987
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
--
作者：
W. Cole;S. Denardo;C. Meares;M. Mccall;G. Denardo;A. Epstein;H. O'Brien;M. K. Moi
通讯作者：
W. Cole;S. Denardo;C. Meares;M. Mccall;G. Denardo;A. Epstein;H. O'Brien;M. K. Moi
影响因子：
2.9
作者：
MEARES, CF;MCCALL, MJ;MCTIGUE, M
通讯作者：
MCTIGUE, M
大鼠肝脏碘甲状腺原氨酸单脱碘酶。
DOI：
--
发表时间：
1986
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Koehrle,J;Auf'mkolk,M;Rokos,H;Hesch,RD;Cody,V
通讯作者：
Cody,V