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《Chinese Journal of Medical Imaging Technology》 2008-01
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Studies on distribution and imaging of ~(131)Ⅰ-labelled RGD peptide in mice bearing tumors

LIU Hong-jie~1 WANG Rong-fu~(1*)ZHANG Chun-li~1 YAN Ping~1 FU Zhan-li~1 ZHANG Xu-chu~1 GUO Feng-qin~1 LIU Meng~1 YU Ming-ming~1 DI Li-juan~1 CUI Yong-gang~1 DING Yi~2 (1.Department of Nuclear Medicine,Peking University First Hospital,Beijing 100034,China; 2.Institute of Urology,Peking University,Beijing 100034,China)  
Objective Due to the selective expression of theαvβ3 integrin in tumors,radiolabelled arginine-glycine-aspartic (RGD)peptides are attractive candidates for tumor targeting.Minor modification of these peptides could have a major im- pact on in vivo characteristic.By studying the distribution and imaging of ~(131)Ⅰlabelled cyclic RGD(cRGD)peptide in mice bearing melanoma,we will discuss the possibility of ~(131)Ⅰ-cRGD peptide as tumor receptor radiotracer.Methods cRGD pep- tide was labelled with ~(131)Ⅰby ChT method under the optimum labelling conditions.~(131)Ⅰ-cRGD peptide was injected into the mice via a vein of mouse tail.The percent injected dose per gram(ID%/g)of different organs and T/NT ratios were meas- ured and calculated.The data was analysed with statistical software of SPSS 12.0.The mice were imaged by SPECT.Re- suits The labelling efficiency and the radiochemical purity of 1311-cRGD peptide reached 90% and 99%,respectively.In dis- tribution,higher radioactivity was found in blood,kidney and bladder,and lower radioactivity in small intestine,liver and musule; 24 hour postinjection,T/M=6.34,and T/B=1.1.The image of tumor was identified at 1 hour post injection of ~(131)Ⅰ-cRGD.Images demonstrated increased ~(131)Ⅰ-cRGD peptide uptake in the tumor after injection 1 to 24 hours gradually. The ~(131)Ⅰ-cRGD peptide uptake in the tumor showed obviously lower when pretreated with cRGD peptide(P0.05).Conclu- sion cRGD peptide could be labelled with ~(131)Ⅰeffectively.~(131)Ⅰ-cRGD peptide accumulated in the tumor after injection via tail vein and its uptake in the tumor showed obviously lower when pretreated with cRGD peptide.The high specificity of ~(131)Ⅰ- cRGD peptide suggested it may be a new promising tumor receptor radiotracer.
【Fund】: “973”项目(2006CB705705-1);; “985”二期项目(985-2-056);; 北京大学第一医院科研基金项目
【CateGory Index】: R73-3
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【Citations】
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1 TANG Lin YU Junfeng ZHENG Mingqiang XIA Jiaoyun YIN Duanzhi (Shanghai Institute of Applied Physics, the Chinese Academy of Sciences, Shanghai 201800, China);Radiolabeling and biodistribution of RGD peptide with ~(188)Re-tricarbonyl complex[J];核技术;2006-06
【Co-citations】
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1 MA Yu-fei1,2,YU Jun-feng1,ZHANG Lan1,HAN Yan-jiang1,2,SHEN Hua1,YIN Duan-zhi1(1.Shanghai Institute of Applied Physics,Chinese Academy of Sciences,Shanghai 201800,China;2.Graduate School of the Chinese Academy of Sciences,Beijing 100049,China);Radiolabeling of RGD Containing Peptide by ~(188)Re and Its Biodistribution[J];同位素;2010-02
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1 YAO Ning;WANG Rong-fu;YAN Ping;ZHANG Chun-li;CHEN Xue-qi;HAO Pan;MA Chao;Department of Nuclear Medicine,Peking University First Hospital;;Study on pharmacokinetics and acute toxicity of new molecular probe ~(99m)Tc-RRL[J];中国临床药理学杂志;2015-16
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