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乳腺癌是常见的恶性肿瘤, 其早期诊断对治疗方案的选择具有重要意义。雌激素受体(estrogen receptor, ER)是乳腺癌发生、发展过程中最为重要的分子生物学标志物[1]。目前, 测定ER的方法主要以肿瘤标本免疫组化法为代表, 但该法为有创、离体测定, 存在取材难等诸多因素的影响和限制, 其对临床内分泌治疗疗效的预测也不够完美。18F-16α-17β-氟雌二醇(18F-16α-17β-fluoroestradiol, 18FFES)是一种雌激素类似物, 能够特异性地与ER结合, 能动态、定量、无创地反映肿瘤ER的生物活性[2-3], 因此, 18F-FES受体显像可为临床提供乳腺癌组织及转移灶内癌细胞的ER分布、密度变化及活动状态等方面的信息, 对于乳腺癌患者的早期诊断、是否采用激素治疗方案及其疗效评估等具有非常重要的价值。18F-FES PET受体显像有望成为比18F-FDG肿瘤代谢显像技术更具有特异性的方法。国外已有文献报道18F-FES的合成过程和方法, 但其步骤较为繁琐复杂[4-6]; 国内也有少量相关报道, 但未见高产率自动化合成的报道[7]。本研究对18FFES的自动化合成进行了探索。
雌激素受体显像剂18F-16α-17β-氟雌二醇的自动化合成
Automated synthesis of the estrogen receptors imaging agent 18F-FES
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摘要:
目的 使用自动化合成装置Tracerlab FXFN,制备雌激素受体显像剂18F-16α-17β-氟雌二醇(18F-FES)。 方法 通过两步反应制备18F-FES:①18F-和3-O-(甲氧甲基)-16, 17-O-磺酰基-16-表雌二醇发生亲核取代反应;②生成物经HCl水解,重复两次后得到产物18F-FES。 结果 18F-FES的合成总时间约80 min,放化产率约为10%,放化纯度大于95%。 结论 整个合成过程自动化完成,操作简便,18F-FES毒性小,对人安全,体外较稳定,有望成为安全、有效的雌激素受体显像剂。 -
关键词:
- 18F-16α-17β-氟雌二醇 /
- 自动化合成
Abstract:Objective 18F-16α-17β-fluoroestradiol(18F-FES), an estrogen receptors imaging agent, is synthesized with Tracerlab FXFNsystem. Methods 18F-FES is obtained by two steps reactions, including the nucleophilic displacement reaction of no-carrier-added18F-fluoride with 3-O-methoxymethyl-16, 17-O-sulfuryl-16-epiesteriol, then the intermediate is evaporated and hydrolyzed with HCl and finally gives18F-FES. Results The synthesis of18F-FES can be completed in about 80 min.The radiochemical yield and radio-chemical purity are about 10%and 95%respectively. Conclusion The procedure ofsynthesis is simple and automatical.18FFES has an extremely lowtoxicity, which suggests that18F-FES may be a safe and effective estrogen receptors imagingagent. -
Key words:
- 18F-16α-17β-fluoroestradiol /
- Automated synthesis
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