点头
体内
化学
体外
点头老鼠
药代动力学
间隙
动力学
药理学
离体
生物化学
生物
医学
泌尿科
物理
生物技术
基因
量子力学
作者
Marc Pretze,Prama Pallavi,Mareike Roscher,Sarah Klotz,Julio Caballero,Uta Binzen,Wolfgang Greffrath,Rolf‐Detlef Treede,Martin C. Harmsen,Mathias Hafner,Benito Yard,Carmen Wängler,Björn Wängler
标识
DOI:10.1021/acs.jmedchem.6b01191
摘要
To mitigate pretransplantation injury in organs of potential donors, N-octanoyl dopamine (NOD) treatment might be considered as it does not affect hemodynamic parameters in braindead (BD) donors. To better assess optimal NOD concentrations for donor treatment, we report on the fast and facile radiofluorination of the NOD-derivative [18F]F-NOD [18F]5 for in vivo assessment of NOD's elimination kinetics by means of PET imaging. [18F]5 was synthesized in reproducibly high radiochemical yields and purity (>98%) as well as high specific activities (>20 GBq/μmol). Stability tests showed no decomposition of [18F]5 over a period of 120 min in rat plasma. In vitro, low cell association was found for [18F]5, indicating no active transport mechanism into cells. In vivo, [18F]5 exhibited a fast blood clearance and a predominant hepatobiliary elimination. As these data suggest that also NOD might be cleared fast, further pharmacokinetic evaluation is warranted.
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