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利用18F标记的生长抑素类似物与一些肿瘤组织中的高表达的生长抑素受体(SSTR)的特异性地结合,可对肿瘤进行显像诊断。生长抑素类似物糖基化修饰后可改善其体内药代动力学特性,降低肝胆等正常组织的摄取,提高对肿瘤的靶向性。为开发一种能够用于生长抑素受体阳性肿瘤诊断的18F标记糖基化生长抑素类似物,本文用Al18F复合物和偶联了螯合剂N O T A的糖基化生长抑素类似物c-Gluc-Lys(NOTA)-TOCA通过螯合反应快速制备了c-GlucLys([Al18F]NOTA)-TOCA,放化合成时间为25~30 min,标记率为73%,最终产品经HLB柱纯化后放化纯大于95%。
Tumors can be diagnostically diagnosed using 18F-labeled somatostatin analogs specifically binding to a highly expressed somatostatin receptor (SSTR) in some tumor tissues. Glycosylation of somatostatin analogues can improve its in vivo pharmacokinetic properties, reduce the uptake of normal tissues such as liver and gallbladder, and improve the targeting of tumors. To develop an 18F-labeled glycosylated somatostatin analog that can be used in the diagnosis of somatostatin receptor-positive tumors, we used the Al 18F complex and the glycosylated somatostatin analogue c- Gluc-Lys (NOTA) -TOCA was rapidly prepared by chelation reaction of c-GlucLys ([Al18F] NOTA) -TOCA, radiochemical synthesis time was 25 ~ 30 min, labeling rate was 73%, the final product was purified by HLB column Radiochemical pure greater than 95%.