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Biodistribution and metabolism of 11C-labeled Kendine 91 in mice and rats

机译:11C标记的Kendine 91在小鼠和大鼠中的生物分布和代谢

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摘要

The biodistribution pattern of [ 11C]Kendine 91 (a novel HDAC inhibitor) after IV administration has been evaluated using Positron Emission Tomography (rats) and gamma counting of dissected tissues (rats and mice) at different doses (1μg/kg and 10.0mg/kg). Metabolism in mice plasma has been also investigated by radio-HPLC. Obtained results (fast accumulation in lungs, heart, kidneys and liver; lower uptake in pancreas and muscle) are in concordance with previously reported results using HPLC/MS-MS. Plasma analysis studies showed a fast metabolism of the radiotracer.
机译:已经使用正电子发射断层扫描(大鼠)和不同剂量(1μg/ kg和10.0mg / kg)的解剖组织(大鼠和小鼠)的γ计数,评估了静脉给药后[11C] Kendine 91(一种新型的HDAC抑制剂)的生物分布模式。公斤)。还已经通过放射-HPLC研究了小鼠血浆中的代谢。获得的结果(在肺,心脏,肾脏和肝脏中快速积累;在胰腺和肌肉中的摄取降低)与先前报道的使用HPLC / MS-MS的结果一致。血浆分析研究表明放射性示踪剂快速代谢。

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