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| 1 | Preparation and biodistribution of ^(99)Tc^m-PIDP as bone imaging agent显示文摘A novel zoledronic acid derivative,1-hydroxy-2-(2-propyl-1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid (PIDP), was synthesized by three-step reactions from 2-propyl-1H-imidazole. It was labeled with 99Tcm in conditions of 0.1 mg SnCl2.2H2O at pH 6.0 and 99TcmO4? in aqueous solution for 20 min at room temperature. The labeling yield and radiochemical purity of 99Tcm-PIDP are both higher than 95%. The biodistribution results show that the bone uptake is up to 8.47% ID/g which is the maximum of bone uptake at 30 min after injection of 99Tcm-PIDP in mice. The pharmacokinetic parameters can be estimated from the exponential equation of C=59.565e-11.307t+2.069e-1.211t. The clear bone image of rabbit was obtained at 120 min after injection of 99Tcm-PIDP. The results indicate that 99Tcm-PIDP has highly selective uptake in the skeletal and low uptake, rapid clearance in soft tissues, so it would be a potential novel bone imaging agent. | CHEN Chuanqing LUO Shineng LIN Jianguo YANG Min YE Wanzhong QIU Ling SANG Guangming XIA Yongmei | 2009 | Nuclear Science and Techniques2009，20，5： | 6 |
| 2 | Syntheses of haptens and hapten-protein conjugates for insecticide propoxur and cyhalothrin显示文摘A facile procedure was described for the hapten design of the N-methylcarbamate insecticide propoxur.Two new haptens of propoxur(hapten 1a and hapten 1b) were synthesized by introducing appropriate spacers in the pesticide aromatic moiety of the analyte molecular structure.First,the propoxur reacted with nitric acid to yield the intermediate product.Then hapten 1a was prepared via the reduction of the intermediate product,and hapten 1b was formed by the acylation of hapten 1a with succinic anhydride.In addition,we have also developed a simple method to prepare hapten 2 for the pyrethroid insecticide cyhalothrin,which only requires two steps including the reactions of nitration and reduction.Three haptens were coupled to carrier proteins to prepare the corresponding artificial antigens.The molecular structures of these three haptens were identified by 1H NMR and MS,and those of the artificial antigens were confirmed by UV-vis. | Sang, GuangMing Luo, ShiNeng Lin, JianGuo Qiu, Ling Chen, ChuanQing Yang, HaiLin Xia, YongMei | 2010 | Science China Chemistry2010，53，5： | 3 |
| 3 | Insulinoma imaging with glucagon-like peptide-1 receptor targeting probe 18 F-FBEM–Cys 39 -exendin-4显示文摘 | Yuping Xu Donghui Pan Qing Xu Chen Zhu Lizhen Wang Fei Chen Runlin Yang Shineng Luo Min Yang | 2014 | Journal of Cancer Research and Clinical Oncology2014，，9： | 1 |
| 4 | Preparation and preliminary biological evaluation of ^(99)Tc^m-TADP as bone imaging agent显示文摘TADP, 2-(1H-1,2,4-triazol-1-yl)-1-hydroxyethane-1,1-diphosphonic acid, was synthesized by three step reactions from the raw material 1H-1,2,4-triazole. Tcm-TADP was prepared with 5 mg TADP at pH 7.0 by joining 99 99TcmO4 with SnCl2·2H2O in aqueous solution for 10 min at room temperature. Both labeling yield and radiochemical - purity of Tcm-TADP were more than 95%. The biodistribution in rats and bone scan in rabbits were also studied. The 99 uptake of organ was expressed as %ID/g. The results showed that the bone uptake is up to 17.17%ID/g which is the maximum of bone uptake at 30 min after injection of Tcm-TADP in rats, bone-to-muscle and bone-to-blood uptake 99 ratios were 61.32 and 13.21, respectively. The clear bone image of rabbit was obtained at 120 min after injection of 99Tcm-TADP and clearance in soft tissue was visible. The preparation of 99Tcm-TADP was convenient and 99Tcm-TADP exhibited high uptake in bone, and it would be a potential new bone imaging agent. | YAN Xiaohong LUO Shineng NIU Guosai YE Wanzhong YANG Min WANG Hongyong XIA Yongmei | 2008 | Nuclear Science and Techniques2008，19，3： | 1 |
| 5 | Study on the reaction kinetics of ^(99)Tc^m-labeled BIDP显示文摘A novel zoledronic acid derivative,1-hydroxy-2-(2-butyl-1H-imidazole-1-yl)-ethylidene-l,l- diphosphonic acid(BIDP),was synthesized and labeled with ^(99)Tc^m.The detailed kinetic study on the labeling reaction between BIDP and ^(99)Tc^m was carried out.The results indicated that the reaction rate constants k were 0.0258,0.0268, 0.0305,0.0323,0.0351 and 0.0384 min^(-1)at 0℃,5℃,10℃,15℃,20℃and 25℃,respectively.From the Arrhenius equation k=A·e^(-E_Δ/(RT)),the activation energy E_a of the labeling reaction was calculated to be 10.45 kJ/mol.And the correlation between k and temperature(T)was also deduced as In k=-1258.8×(l/T)+0.9531.In addition,it was found that in order to get a high radiolabeling yield(RLY)(>90%),the reaction temperature must be up to 12℃. | LIN Jianguo WANG Yan LUO Shineng QIU Ling ZHAI Haozhen | 2011 | Nuclear Science and Techniques2011，22，3： | 0 |
| 6 | Semi-automated synthesis,validation and microPET imaging of ^(18)F-FP-DTBZ as a vesicular monoamine transporter ligand显示文摘This work was to develop a semi-automated synthesis of 18F-9-fluoropropyl-9-desmethyl-DTBZ (18F-FP-DTBZ) and validate its potential as a vesicular monoamine transporter 2 (VMAT2) ligand.18F-FP-DTBZ was synthesized by a semi-automated procedure in a 21-35% yield without decay correction and with a radiochemical purity of >98%.Bioistribution in rats exhibited a favorable brain uptakes of the ligand (0.31±0.04 ID% at 60min post injection,n=8).The highest radioactivity located in VMAT2 enriched striatal tissue.The target-to-nontarget ratio (striatum/cerebellum,ST/CB) was 4.81±0.84.Blocking studies implied that striatum uptake could be blocked by DTBZ (a VMAT2 inhibitor) but could not by CFT (a dopamine transporter inhibitor).MicroPET imaging with 18F-FP-DTBZ in normal rats gave high quality images in which high radioactivity were observed in the striatal tissue.Time-and-activity curves revealed good retention in the target (striatum) and rapid clearance in the background (cerebellum),which resulted in a maximum ST/CB ratio of 5.08±0.81 (n=3) in 80-120min.By contrast,the 6-hydroxydopamine unilateral lesioned rats gave asymmetrical striata images with higher 18F-FP-DTBZ concentration on the unlesioned side (unlesioned-ST/CB=5.21±0.38,n=3) than the lesioned (lesioned-ST/CB=2.34±0.51).The results validated that 18F-FP-DTBZ is a favorable PET ligand binding to VMAT2. | CHEN Zhengping LIU Chunyi LI xiaomin TANG Jie TAN Cheng HUANG Hongbo YU Huixin LUO Shineng | 2012 | Nuclear Science and Techniques2012，23，1： | 0 |
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