趋化因子受体CXCR4拮抗剂AMD3100的合成及^99Tcm标记

趋化因子受体CXCR4在多数恶性肿瘤中高表达，其小分子拮抗剂AMD3100可用于肿瘤治疗。以N，N-二（3-氨丙基）乙基乙胺为原料合成了AMD3100，并用放射性金属核素^99Tcm标记制备^99Tcm-AMD3100，研究其在正常NH小鼠体内生物分布及荷Hep—G2肝癌鼠SPECT显像。结果显示，以N，N-二（3-氨丙基）乙基乙胺为原料，合成AMD3100总的合成效率为5．8％。^99Tcm-AMD3100的标记率大于98％。生物分布结果表明，CXCR4高表达的肝组织放射性摄取较高。显像结果表明，荷Hep—G2肝癌组织可浓集放射性。以上结果表明，^99Tcm-AMD3100是一种潜在的肿瘤C...

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Bibliographic Details
Published in同位素 Vol. 26; no. 3; pp. 158 - 162
Main Author 桂媛 徐志宏 张晓军 张书文 刘健 田嘉禾 张锦明
Format Journal Article
LanguageChinese
Published 江苏华益科技有限公司,江苏常熟,215522%中国人民解放军总医院核医学科 北京 100853 2013
Subjects
99Tcm
AMD3100
CXCR4
趋化因子受体
99Tcm
CXCR4
趋化因子受体
chemokines
AMD3100
Online AccessGet full text
ISSN1000-7512
DOI10.7538/tws.2013.26.03.0158

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Summary:趋化因子受体CXCR4在多数恶性肿瘤中高表达，其小分子拮抗剂AMD3100可用于肿瘤治疗。以N，N-二（3-氨丙基）乙基乙胺为原料合成了AMD3100，并用放射性金属核素^99Tcm标记制备^99Tcm-AMD3100，研究其在正常NH小鼠体内生物分布及荷Hep—G2肝癌鼠SPECT显像。结果显示，以N，N-二（3-氨丙基）乙基乙胺为原料，合成AMD3100总的合成效率为5．8％。^99Tcm-AMD3100的标记率大于98％。生物分布结果表明，CXCR4高表达的肝组织放射性摄取较高。显像结果表明，荷Hep—G2肝癌组织可浓集放射性。以上结果表明，^99Tcm-AMD3100是一种潜在的肿瘤CXCR4表达显像剂。
Bibliography:chemokines; CXCR4 ; AMD3100 ; 99 Tcm
11-2566/TL
Most of human tumors over-express CXCR4. AMD3100, a nonpeptide antagonist for CXCR4 receptor, can be used for therapy of those tumors. It was found that metal ion complex, such as Cuz＋ , with AMD3100 enhanced its binding affinity to the receptor 10-fold higher as compared to AMD3100 alone. AMD3100 was synthesis from 3-aminopropyl ethyl- ene diamine. 99Tcm-AMD3100 was labeled directly. Biodistribution studies were carried out in NH mice. SPECT imaging was performed in Hep-G2 tumor bearing mouse. The synthet- ic yield was 5.8% from 3-aminopropyl ethylene diamine to AMD3100. The labeling yield of 99Tcm-AMD3100 was over 98%. Biodistribution studies showed high accumulation of radio- tracer in liver which had high-expression of CXCR4. SPECT imaging results showed that uptake in Hep-G2 tive candidate for CR4. tumor was high. The further development results showed that 99Tcm-AMD3100 was an attrac- of SPECT radiotracer potentially suitable for CX
GUI Yuan ,XU Zhi-hong1 , Z
ISSN:1000-7512
DOI:10.7538/tws.2013.26.03.0158