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[11C]palmitate kinetics across the splanchnic bed in arterial, portal and hepatic venous plasma during fasting and euglycemic hyperinsulinemia.空腹和正常血糖高胰岛素血症期间,动脉血、门静脉血和肝静脉血浆中[11C]棕榈酸在脏床的动力学。
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Polyethylene glycol-phosphatidylethanolamine conjugate (PEG-PE)-based mixed micelles: some properties, loading with paclitaxel, and modulation of P-glycoprotein-mediated efflux.基于聚乙二醇-磷脂酰乙醇胺共轭物(PEG-PE)的混合胶束:一些性质、紫杉醇负载及P-糖蛋白介导的外排调节
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Validation of 18F-fluoro-4-thia-palmitate as a PET probe for myocardial fatty acid oxidation: effects of hypoxia and composition of exogenous fatty acids.18F-氟-4-硫代棕榈酸酯作为心肌脂肪酸氧化PET探针的验证:缺氧及外源性脂肪酸组成的影响
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用[18F]氟代二棕榈酸酯([18F]FDP)放射性标记的长循环脂质体。

Long-circulating liposomes radiolabeled with [18F]fluorodipalmitin ([18F]FDP).

作者信息

Marik Jan, Tartis Michaelann S, Zhang Hua, Fung Jennifer Y, Kheirolomoom Azadeh, Sutcliffe Julie L, Ferrara Katherine W

机构信息

Department of Biomedical Engineering, University of California Davis, Davis, CA 95616, USA.

出版信息

Nucl Med Biol. 2007 Feb;34(2):165-71. doi: 10.1016/j.nucmedbio.2006.12.004.

DOI:10.1016/j.nucmedbio.2006.12.004
PMID:17307124
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1849971/
Abstract

Synthesis of a radiolabeled diglyceride, 3-[(18)F]fluoro-1,2-dipalmitoylglycerol [[(18)F]fluorodipalmitin ([(18)F]FDP)], and its potential as a reagent for radiolabeling long-circulating liposomes were investigated. The incorporation of (18)F into the lipid molecule was accomplished by nucleophilic substitution of the p-toluenesulfonyl moiety with a decay-corrected yield of 43+/-10% (n=12). Radiolabeled, long-circulating polyethylene-glycol-coated liposomes were prepared using a mixture of 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, cholesterol, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethyleneglycol)-2000] ammonium salt (61:30:9) and [(18)F]FDP with a decay-corrected yield of 70+/-8% (n=4). PET imaging and biodistribution studies were performed with free [(18)F]FDP and liposome-incorporated [(18)F]FDP. Freely injected [(18)F]FDP had the highest uptake in the liver, spleen and lungs. Liposomal [(18)F]FDP remained in blood circulation at near-constant levels for at least 90 min, with a peak concentration near 2.5%ID/cc. Since [(18)F]FDP was incorporated into the phospholipid bilayer, it could potentially be used for radiolabeling a variety of lipid-based drug carriers.

摘要

研究了放射性标记的甘油二酯3-[(18)F]氟-1,2-二棕榈酰甘油[[(18)F]氟代二棕榈精([(18)F]FDP)]的合成及其作为放射性标记长循环脂质体试剂的潜力。通过对甲苯磺酰基部分的亲核取代将(18)F掺入脂质分子中,校正衰变后的产率为43±10%(n = 12)。使用1,2-二棕榈酰-sn-甘油-3-磷酸胆碱、胆固醇、1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-N-[甲氧基(聚乙二醇)-2000]铵盐(61:30:9)和[(18)F]FDP的混合物制备放射性标记的长循环聚乙二醇包被脂质体,校正衰变后的产率为70±8%(n = 4)。用游离的[(18)F]FDP和脂质体掺入的[(18)F]FDP进行PET成像和生物分布研究。自由注射的[(18)F]FDP在肝脏、脾脏和肺中的摄取最高。脂质体[(18)F]FDP在血液循环中至少90分钟保持近乎恒定的水平,峰值浓度接近2.5%ID/cc。由于[(18)F]FDP被掺入磷脂双层中,它有可能用于放射性标记多种基于脂质的药物载体。