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放射性标记的[DTPA0]奥曲肽和[DOTA0,Tyr3]奥曲肽的内化:用于生长抑素受体靶向闪烁显像和放射性核素治疗的肽

Internalization of radiolabelled [DTPA0]octreotide and [DOTA0,Tyr3]octreotide: peptides for somatostatin receptor-targeted scintigraphy and radionuclide therapy.

作者信息

De Jong M, Bernard B F, De Bruin E, Van Gameren A, Bakker W H, Visser T J, Mäcke H R, Krenning E P

机构信息

Department of Nuclear Medicine, University Hospital Dijkzigt, Rotterdam, The Netherlands.

出版信息

Nucl Med Commun. 1998 Mar;19(3):283-8. doi: 10.1097/00006231-199803000-00013.

Abstract

We compared the internalization of [90Y-DOTA0,Tyr3]octreotide and [111In-DOTA0,Tyr3]octreotide with that of [125I-Tyr3]octreotide and [111In-DTPA0]octreotide in the subtype 2 somatostatin receptor (sst2)-positive rat pancreatic tumour cell lines CA20948 and AR42J and in the somatostatin receptor-negative human anaplastic thyroid tumour cell line ARO. We demonstrated that [111In-DTPA0]octreotide, [90Y-DOTA0,Tyr3]octreotide and [111In-DOTA0,Tyr3]octreotide are internalized by a receptor-specific, time- and temperature-dependent process. The amount of [90Y-DOTA0,Tyr3]octreotide internalized was higher than that of [111In-DOTA0,Tyr3]octreotide and [111In-DTPA0]octreotide.

摘要

我们比较了[90Y-DOTA0,Tyr3]奥曲肽、[111In-DOTA0,Tyr3]奥曲肽与[125I-Tyr3]奥曲肽、[111In-DTPA0]奥曲肽在2型生长抑素受体(sst2)阳性大鼠胰腺肿瘤细胞系CA20948和AR42J以及生长抑素受体阴性的人未分化甲状腺肿瘤细胞系ARO中的内化情况。我们证明,[111In-DTPA0]奥曲肽、[90Y-DOTA0,Tyr3]奥曲肽和[111In-DOTA0,Tyr3]奥曲肽通过受体特异性、时间和温度依赖性过程内化。[90Y-DOTA0,Tyr3]奥曲肽的内化量高于[111In-DOTA0,Tyr3]奥曲肽和[111In-DTPA0]奥曲肽。

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