核化学与放射化学2012，Vol.34Issue(3)：157-165,9.
n-Gluc-Lys([Al18F] NOTA )-TOCA的制备和初步生物学评价
Preparation and Preliminary Biological Evaluation of n-Gluc-Lys([Al18F]NOTA)-TOCA
郭飞虎 1陈玉清 2刘婷 2陈宝军 3梁积新 2徐琪 2邱芊 4陈大明 4杜进2
作者信息
- 1. 中国原子能科学研究院同位素研究所,北京102413
- 2. 原子高科股份有限公司,北京102413
- 3. 环境保护部核与辐射安全中心政策法规研究所,北京100082
- 4. 杭州中肽生化有限公司,浙江杭州310018
- 折叠
摘要
Abstract
Octreotide and their derivatives can specificially bind with somatostatin receptor (SSTR) which is usually over-expressed on many tumor cells. So 18F labeled octreotide and their derivatives can be used for the diagnosis and evaluation of therapeutic efficacy of SSTR positive tumors. In order to explore a novel PET probe for diagnosis of SSTR positive tumors, the n-Gluc-Lys([Al18 F]NOTA)-TOCA was radio-synthesized fast and efficiently using the chelation reaction of n-Gluc-Lys(NOTA)-T0CA with Al18 F moiety. N-Gluc-Lys ([A118F]NOTA)-TOCA was a glycosylated octreotide derivative combined with 1,4,7-tri-azacyclononane-l,4,7-triacetic acid (NOT A). The labeling efficiency of n-Giuc-Lys([Al18F] NOTA)-TOCA is 69% and the total synthesis time is 25-30 min. The radiochemical purity is over 95% after HLB column purification. The stability in vitro is excellent, and the hydro-philicity is highdg P= -4. 20±. 09(n = 3)). Biodistribution studies in normal mice at 2 h after injection show that the uptake of n-Gluc-Lys([A18F]NOTA)-TOCA in kidney is high ((13. 83±3. 52)%ID/g(n = 5)) and the uptake in liver and bone is low. The uptake in sama-tostatin pancreas receptor express is high, and the background of blood and muscle is low. These preliminary results provide some experimental basis for further study of Al18 F complex labeled octreotide and their analogues as tumor probes for the diagnosis of SSTR-posi-tive tumors.关键词
生长抑素(SST)/奥曲肽/Al18F复合物/正电子发射计算机断层显像(PET)Key words
somatostatin(SST)/octreotide) aluminum fluoride complex (A11SF)/positron emission computed tomography(PET)分类
医药卫生引用本文复制引用
郭飞虎,陈玉清,刘婷,陈宝军,梁积新,徐琪,邱芊,陈大明,杜进..n-Gluc-Lys([Al18F] NOTA )-TOCA的制备和初步生物学评价[J].核化学与放射化学,2012,34(3):157-165,9.
