Synthesis and preliminary evaluation of carbon-11-meta-hydroxyephedrine: a false transmitter agent for heart neuronal imaging.
Synthesis and preliminary evaluation of carbon-11-meta-hydroxyephedrine: a false transmitter agent for heart neuronal imaging.
复制标题
DOI：
--
复制
发表时间：
1990-08
期刊：
影响因子：
--
通讯作者：
K. Rosenspire;M. Haka;M. V. Dort;D. Jewett;D. Gildersleeve;M. Schwaiger;D. Wieland
中科院分区：
文献类型：
--
作者：
K. Rosenspire;M. Haka;M. V. Dort;D. Jewett;D. Gildersleeve;M. Schwaiger;D. Wieland
碳-11-间羟麻黄碱是一种新的心脏交感神经示踪剂。在二甲基甲酰胺/二甲基亚砜中，间羟胺与[11 C]碘甲烷直接N-甲基化合成了碳-11-间羟基麻黄碱，并通过半制备反相HPLC纯化。总合成时间为轰击结束后45分钟。以40%-50%的校正放射化学产率生产碳-11-间羟基麻黄碱，比活度为900 Ci/mmol。常规放射化学和化学纯度分别为95%和98%。大鼠的生物分布研究显示心肌摄取较高。用地昔帕明（一种已知选择性阻断神经元摄取的药物）预处理，导致心肌中示踪剂蓄积减少92%。豚鼠代谢研究显示，静脉注射后30分钟，心脏组织中的代谢物少于5%，表明[11 C]间羟基麻黄碱适用于动力学建模。这些初步结果支持这种新的示踪剂作为心脏神经元成像的临床试剂。
Carbon-11-meta-hydroxyephedrine is a new radiotracer developed for mapping the sympathetic nerves of the heart. Carbon-11-meta-hydroxyephedrine is synthesized by direct N-methylation of metaraminol with [11C]methyl iodide in dimethyl formamide/dimethyl sulfoxide and purified by semi-preparative reversed-phase HPLC. Total synthesis time is 45 min from end-of-bombardment. Carbon-11-meta-hydroxyephedrine is produced in 40%-50% corrected radiochemical yield with a specific activity of 900 Ci/mmol. Routine radiochemical and chemical purity are 95% and 98%, respectively. Biodistribution studies in rats show high myocardial uptake. Pretreatment with desipramine, a drug known to selectively block neuronal uptake, results in a 92% decrease in tracer accumulation in the myocardium. Metabolic studies in guinea pigs show less than 5% metabolites in heart tissue 30 min after intravenous injection suggesting that [11C]meta-hydroxyephedrine is suitable for kinetic modeling. These preliminary results support this new tracer as a clinical agent for neuronal imaging of the heart.