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Radiolabeling of lacosamide using highly purified rhenium-188 as a prospective brain theranostic agent 被引量:1
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作者 H.A.El-Sabagh M.I.Aydia +1 位作者 A.M.Amin K.M.El-Azony 《Nuclear Science and Techniques》 SCIE CAS CSCD 2020年第10期105-114,共10页
Rhenium-188 is prospectively effective for both diagnosis and radiotherapy as it appropriately emits gamma rays and beta particles.Lacosamide(LCM)is a newly approved antiepileptic medication for focal drug-resistant e... Rhenium-188 is prospectively effective for both diagnosis and radiotherapy as it appropriately emits gamma rays and beta particles.Lacosamide(LCM)is a newly approved antiepileptic medication for focal drug-resistant epilepsy.Rhenium-188 was separated with high elution yield and high purity using the new 188W/188Re generator based on the ZrSiW gel matrix.188Re-LCM was prepared with high radiochemical yield and high purity.Biodistribution of 188Re-LCM in normal Swiss albino mice was investigated to determine its utility as a potential brain therapy agent.The 188W/188Re generator was used to obtain 188Re based on the ZrSi188W gel matrix,and the chemical,radiochemical,and radionuclidic purity of the obtained 188Re was determined using inductively coupled plasma optical emission spectrometry(ICP-AES),a paper chromatography technique,and high-purity germanium(HPGe)detection,respectively,to assess its validity for LCM labeling.Various factors,such as the pH,reaction time,and LCM quantity,were therefore studied in order to improve the yield and purity of 188Re-LCM,as determined by various chromatographic techniques such as electrophoresis,thin layer chromatography(TLC),and highpressure liquid chromatography(HPLC).188Re was obtained with a high elution yield(75±3%)and a low 188W breakthrough(0.001±0.0001%).The maximum radiochemical yield of 188Re-LCM(87.5±1.8%)was obtained using 50 ll LCM(4 mM),250 ll stannous chloride(4.4 mM)at pH 4,100 ll 188Re(37 MBq),within 30 min,at room temperature(25±3C),as determined by TLC,electrophoresis,and HPLC techniques.Biodistribution analysis showed that 188Re-LCM was primarily localized in the brain(5.1%)with a long residence time(240 min). 展开更多
关键词 LACOSAMIDE 188Re 188W/188Re generator radiolabelING
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Expression and radiolabeling of Cas9 protein
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作者 Qing-Long Yan Hua-Ting Kong +7 位作者 Kai Xia Yu Zhang Ali Aladlbahi Ji-Ye Shi Li-Hua Wang Chun-Hai Fan Yun Zhao Ying Zhu 《Nuclear Science and Techniques》 SCIE CAS CSCD 2017年第1期74-79,共6页
As a robust platform for genome editing,CRISPR/Cas9 is currently being explored for engineering biology or therapeutics,yet means for quantitative detection of Cas9 proteins remain to be fully realized.Here,we express... As a robust platform for genome editing,CRISPR/Cas9 is currently being explored for engineering biology or therapeutics,yet means for quantitative detection of Cas9 proteins remain to be fully realized.Here,we expressed Cas9 proteins and developed a novel detection method that traced Cas9 based on radiolabeled iodine.Through optimizing the reaction conditions of reaction time,temperature and cycles,we obtained ^(125)I-Cas9 of high labeling yield.The prepared ^(125)I-Cas9 was stable in various media and preserved excellent genome editing efficiency.Thus,our strategy provides a convenient and efficient tool for further tracing biological behaviors of Cas9 proteins in living systems. 展开更多
关键词 Cas9 radiolabelING 125I LABELING YIELD STABILITY
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A NEW BIFUNCTIONAL CHELATING AGENT α,ε-N,N'-BIS(L-CYSTEINYL)-L-LYSINE FOR RADIOLABELLING OF MONOCLONAL ANTIBODIES WITH TECHNETIUM-99M
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作者 Bi Zhong LI Yuan Fang LIU Yong Hui WU Department of Technical PhysicsYun Hua YE Department of Chemistry,Peking University,Beijing 100871 《Chinese Chemical Letters》 SCIE CAS CSCD 1991年第4期285-288,共4页
α,ε-N,N'-bis(L-cysteinyl)-L-lysine was synthesized and char- acterized for the first time.It was then employed as a bifunctional chelating agent to chelate technetium-99m and subsequently conjugated to fragment ... α,ε-N,N'-bis(L-cysteinyl)-L-lysine was synthesized and char- acterized for the first time.It was then employed as a bifunctional chelating agent to chelate technetium-99m and subsequently conjugated to fragment F(ab')_2 of anti-gastric tumor monoclonal antibody 3G9.The radiolabelled antibody was satisfactorily stable and immunoreactive. 展开更多
关键词 A NEW BIFUNCTIONAL CHELATING AGENT L-CYSTEINYL L-LYSINE FOR radiolabelLING OF MONOCLONAL ANTIBODIES WITH TECHNETIUM-99M N N BIS
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Radiolabeled FMLF a Valuable Peptide for Diagnostic Imaging
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作者 Fatemeh Keshavarzi Parviz Ashtari 《Journal of Pharmacy and Pharmacology》 2014年第1期70-78,共9页
Molecular imaging techniques are increasingly being used in the localization of disease, the staging of disease and for therapy control. The objective of current study focused on the optimization of synthesis, quality... Molecular imaging techniques are increasingly being used in the localization of disease, the staging of disease and for therapy control. The objective of current study focused on the optimization of synthesis, quality control, in vitro and in vivo evaluation of 123I radiopharmaceuticals based on the chemotactic peptide N-formyl-Met-Leu-Phe. Labeling studies were done both by direct method using chloramine-Y according to Khawli (1989) and indirect method using [125I and 131I] S1B according to Zalutsky (1987). Then, biodistribution studies were performed both in normal mice and the one bearing 50 laL turpentine for 24h, promoted inflammation in right leg. Furthermore, the ability of the labeled peptide conjugate to bind to human polymorph nuclear leukocytes was determined using in vitro assay. With increasing in pl-l, yield of labeled FMLF (N-formyl-Met-Leu-Phe) decreased perhaps because of interaction OH to carboxyl group of SIB. The maximum activity was observed in the right leg which injected with turpentine due to infection and increase in blood circulation. Also, this peptide was conjugated to PMN (Poly morph nuclear) specifically and maximum activity was 66%. The highest absorption of FLMF was seen in kidney, liver, stomach and gut. The small size of this protein causes passing through the glomerular of kidney, so high activity was observed in urine and bladder. 展开更多
关键词 Molecular imaging FLMF radiolabeled peptide.
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Peptides radiolabeled with Re-186/188 and Tc-99m as potential diagnostic and therapeutic agents 被引量:5
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作者 E. GARCíA-GARAYOA R. SCHIBLI P.A. SCHUBIGER 《Nuclear Science and Techniques》 SCIE CAS CSCD 2007年第2期88-100,共13页
Small peptide-based compounds have attracted an enormous interest as carrier molecules to selectively de- liver radionuclides to target tissues, sparing critical normal organs. When looking for "matched pairs&quo... Small peptide-based compounds have attracted an enormous interest as carrier molecules to selectively de- liver radionuclides to target tissues, sparing critical normal organs. When looking for "matched pairs" of radionuclides, suitable for radiolabeling of peptides for diagnosis and therapy, technetium and rhenium represent an almost ideal constellation. The important role of technetium-99m and Re-186/188 is based on the decay characteristics, suitable for tumor diagnosis and therapy. Tc-99m and Re-188 are readily available by either a 99Mo/99mTc or the 188W/188Re ra- dionuclide generator system. Furthermore, technetium and rhenium are chemically related and share structural as well as reactive similarities, which prompt an attractive "matched-pair" situation. This article shows an overview of 99mTc- and 186/188Re-radiolabeled peptides that have been tested for their potential use as imaging and therapeutic agents in oncological diseases. 展开更多
关键词 放射性同位素标记肽类 铼186/188 锝99M 诊断药物 治疗药物
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Synthesis, radiolabeling and biological evaluation of butene amine oxime containing nitrotriazole as a tumor hypoxia marker
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作者 Qiang Zhang Tai-Wei Chu 《Nuclear Science and Techniques》 SCIE CAS CSCD 2016年第2期35-43,共9页
^(99m)Tc-BnAO, as a nonnitroaromatic hypoxia marker, is the subject of intensive research in recent years. In this study, a butene amine oxime–nitrotriazole(Bn AO–NT)was synthesized and radiolabeled with ^(99m)Tc in... ^(99m)Tc-BnAO, as a nonnitroaromatic hypoxia marker, is the subject of intensive research in recent years. In this study, a butene amine oxime–nitrotriazole(Bn AO–NT)was synthesized and radiolabeled with ^(99m)Tc in high yield.Cellular uptakes of^(99m)Tc-Bn AO–NT and ^(99m)Tc-Bn AO were tested using murine sarcoma S180 and hepatoma H22 cell lines. The highest hypoxic cellular uptake of^(99m)TcBn AO–NT was 27.11 ± 0.73 and 14.85 ± 0.83 % for the S180 and H22 cell lines, respectively, whereas the normoxic cellular uptake of the complex was about 4–8 % for both cell lines. For^(99m)Tc-Bn AO, the highest hypoxic cellular uptake was 30.79 ± 0.44 and 9.66 ± 1.20 % for the S180 and H22 cell lines, respectively, while the normoxic cellular uptake was about 5 % for both cell lines. Both^(99m)Tc-Bn AO–NT and^(99m)Tc-Bn AO complexes showed hypoxic/normoxic differentials in the two cell lines, but the results were more significant for the S180 cell line. The in vitro results suggested that S180 may be better than H22 cell line in hypoxic biological evaluation of Bn AO complexes. The biodistribution study was tested using a S180 tumor model. The complex^(99m)Tc-Bn AO–NT showed a selective enrichment in tumor tissues: At 4 h, the tumor-to-muscle ratio was 3.79 ± 0.98 and the tumor-to-blood ratio was 2.31 ± 0.34.Compared with the results of ^(99m)Tc-Bn AO, the latter was at the same level. In vitro and in vivo studies demonstrated that ^(99m)Tc-Bn AO–NT could be a hypoxia-sensitive radiotracer for monitoring hypoxic regions in a sarcoma S180 tumor. 展开更多
关键词 细胞缺氧 肿瘤模型 生物学评价 标记 合成 胺肟 丁烯 S180
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Directly radiolabeled phage with spleen-targeting specificity
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作者 SUN Liyan LIANG Kun WANG Xiangyun CHU Taiwei 《Nuclear Science and Techniques》 SCIE CAS CSCD 2011年第4期217-223,共7页
Phage display technique is a powerful approach for discovering new tumor-and organ-targeting ligands,and radiolabeled phage has a potential to analyze the phage-binding sensitivity and specific imaging.In this study,p... Phage display technique is a powerful approach for discovering new tumor-and organ-targeting ligands,and radiolabeled phage has a potential to analyze the phage-binding sensitivity and specific imaging.In this study,phage Ⅱ (the spleen-targeting phage) in mice was isolated after three rounds biopanning,and labeled by 99mTc using mercaptoacetyltriglycine (MAG3) as chelator to evaluate their binding properties in vivo.The amount of phage Ⅱ eluted from spleen was enriched by plague assay each round.99mTc-MAG3-phage Ⅱ showed the less retention in blood at any time point than half that of 99mTc-MAG3-phage Ⅰ (the radiolabeled original Ph.D-12 phage as control).The accumulation in spleen between 99mTc-MAG3-phage Ⅰ and Ⅱ was of different tendency.The highest uptake of 99mTc-MAG3-phage Ⅱ in spleen was 24.80 %ID/g at 30 min;and of 99mTc-MAG3-phage I,30.93% ID/g at 5 min.After circulating 99mTc-MAG3-phage Ⅱ for 120 min,its accumulation in spleen decreased though higher than that of 99mTc-MAG3-phage Ⅰ.In other organs,the 99mTc-MAG3-phage Ⅱ showed low retention and high spleen-to-organ or tissue ratios.In conclusion,the radiolabeled phage Ⅱ is convenient for studying the binding and specificity of spleen-targeting peptides found via phage display in vivo. 展开更多
关键词 噬菌体展示技术 放射性标记 脾脏 异性 MAG3 噬菌体显示 灵敏度 器官
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^(125)I-interleukin-8 radiolabelling and in vivo distribution
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作者 FANWo QIANJian-Hua ZHURan NINPing XUYu-Jie ZHANGYi 《Nuclear Science and Techniques》 SCIE CAS CSCD 2004年第2期111-114,共4页
To study the radioiodinating condition of interleukin-8(IL-8) and observe its biodistribution in mice for understanding the possibility of its application in nuclear medicine, we labelled IL-8 with 125I using Bolton-H... To study the radioiodinating condition of interleukin-8(IL-8) and observe its biodistribution in mice for understanding the possibility of its application in nuclear medicine, we labelled IL-8 with 125I using Bolton-Hunter reagent, and the distributions in mice at 5 min, 30 min, 1h, 6h and 24h after injection of 125I –IL-8 were measured. The blood clearance curve was obtained and fitted with the two-compartment model. The results showed that 125I-IL-8 was obtained with a labeling efficiency of 12.2% ±6.5% and a radiochemical purity of 91.4%±6.5%. Its spe- cific activity was 14.8 kBq/μg IL-8. A fast phase half – life T1/2 of 0.32 h and a slow phase half – life T1/2 of 8.01 h α β were calculated from the blood clearance curve. The uptakes of radioactivities in kidneys and lung had the peaks of 85.87%ID /g and 16.17%ID /g at 30 min after intravenous injection, respectively. The uptakes in liver and spleen were 12.05%ID /g and 8.97%ID /g as the maximum at 5 min after injection. The clearance in blood and other organs was fast. Except for kidneys and lung, 125I –IL-8 was less than 1%ID/ g 24 h after administration. It is concluded that radioiodinated IL-8 is a promising radiopharmaceutical in nuclear medicine, especially for imaging infection. But to enhance the labeling efficiency of radioiodinated IL-8 and to decrease its in vivo deiodination are the subjects neces- sary to be further investigated. 展开更多
关键词 白细胞间介素-8 放射性同位素示踪 生物分布 氨基酸
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A study on indirect radiolabeling of IgG with carrier free ^(188)Re
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作者 ZHANG Xiu-Li, WANG Yong-Xian, LI Jun-Ling, YIN Duan-Zhi (Shanghai Institute of Nuclear Research, the Chinese Academy of Sciences, Shanghai 201800) 《Nuclear Science and Techniques》 SCIE CAS CSCD 2003年第2期131-134,共4页
188Re labeled monoclonal antibodies are potential candidates for use in radioimmunotherapy. S-Bz-MAG3 as a bifunctional chelating agent was used for labeling of IgG with carrier free 188Re by pre-radiolabeling of the ... 188Re labeled monoclonal antibodies are potential candidates for use in radioimmunotherapy. S-Bz-MAG3 as a bifunctional chelating agent was used for labeling of IgG with carrier free 188Re by pre-radiolabeling of the chelating approach. The conjugation conditions were optimized. The stability of 188Re-MAG3-IgG in vitro was high. The results may be useful to the studies of 188Re labeled MAbs for radioimmunotherapy. 展开更多
关键词 ^188RE 单克隆抗体 放射免疫性疗法
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Higher Grain-Filling Rate in Inferior Spikelets of Tolerant Rice Genotype Offset Grain Yield Loss under Post-Anthesis High Night Temperatures
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作者 Nitin SHARMA Bhupinder SINGH +6 位作者 Subbaiyan Gopala KRISHNAN Haritha BOLLINEDI Pranab Kumar MANDAL Milan Kumar LAL Prakash Kumar JHA P.V.Vara PRASAD Anjali ANAND 《Rice science》 SCIE CSCD 2024年第5期572-586,I0059-I0061,共18页
Increased nighttime respiratory losses decrease the amount of photoassimilates available for plant growth and yield. We hypothesized that the increased respiratory carbon loss under high night temperatures(HNT) could ... Increased nighttime respiratory losses decrease the amount of photoassimilates available for plant growth and yield. We hypothesized that the increased respiratory carbon loss under high night temperatures(HNT) could be compensated for by increased photosynthesis during the day following HNT exposure. Two rice genotypes, Vandana(HNT-sensitive) and Nagina 22(HNT-tolerant), were exposed to HNT(4 ℃ above the control) from flowering to physiological maturity. They were assessed for alterations in the carbon balance of the source(flag leaf) and its subsequent impact on grain filling dynamics and the quality of spatially differentiated sinks(superior and inferior spikelets). Both genotypes exhibited significantly higher night respiration rates. However, only Nagina 22 compensated for the high respiration rates with an increased photosynthetic rate, resulting in a steady production of total dry matter under HNT. Nagina 22 also recorded a higher grain-filling rate, particularly at 5 and 10 d after flowering, with 1.5- and 4.0-fold increases in the translocation of ^(14)C sugars to the superior and inferior spikelets, respectively. The ratio of photosynthetic rate to respiratory rate on a leaf area basis was negatively correlated with spikelet sterility, resulting in a higher filled spikelet number and grain weight per plant, particularly for inferior grains in Nagina 22. Grain quality parameters such as head rice recovery, high-density grains, and gelatinization temperature were maintained in Nagina 22. An increase in the rheological properties of rice flour starch in Nagina 22 under HNT indicated the stability of starch and its ability to reorganize during the cooling process of product formation. Thus, our study showed that sink adjustments between superior and inferior spikelets favored the growth of inferior spikelets, which helped to offset the reduction in grain weight under HNT in the tolerant genotype Nagina 22. 展开更多
关键词 high night temperature inferior grain pasting property radiolabeled sugar superior grain
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^(64)Cu radiolabeled nanomaterials for positron emission tomography(PET)imaging 被引量:3
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作者 Xueqian Chen Wenchao Niu +3 位作者 Zhongying Du Yong Zhang Dongdong Su Xueyun Gao 《Chinese Chemical Letters》 SCIE CAS CSCD 2022年第7期3349-3360,共12页
The prevalence of positron emission tomography(PET)imaging has advanced biomedical applications for its ultrahigh sensitivity,deep tissue penetration and quantitative visualization of diseases in vivo.^(64)Cu with ide... The prevalence of positron emission tomography(PET)imaging has advanced biomedical applications for its ultrahigh sensitivity,deep tissue penetration and quantitative visualization of diseases in vivo.^(64)Cu with ideal half-life and decay characteristics has been designed as radioactive probes for disease diagnosis.The currently reported ^(64)Cu-labeled nanomaterials have the advantages of long circulation time in serum,good biocompatibility and mature preparation methods,and have been used in vivo PET imaging,biodistribution and pharmacokinetic monitoring,and imaging guided therapy.At the same time,suitable carrier characteristics and radiolabeling strategies are particularly important in the ^(64)Cu PET imaging process.In this review,we summarize different imaging probe designs and ^(64)Cu radiolabeling strategies,as well as their eventual applications in biomedicine.The potential challenges and prospects of ^(64)Cu labeled nanomaterials are also described,which provides broad prospects for radiolabeling strategies and further applications. 展开更多
关键词 ^(64)Cu Positron emission tomography Chelating agent-free radiolabeling strategies Imaging guided therapy
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一种caspase-3靶向激活型PET分子探针的制备与表征
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作者 张理霞 徐梁 +3 位作者 李惠蓉 梁蓓蓓 林建国 邱玲 《合成化学》 CAS 2023年第3期177-185,共9页
诱导肿瘤细胞凋亡是多种肿瘤治疗方案的作用机制之一,因此检测肿瘤细胞是否产生凋亡已成为评价肿瘤治疗疗效的一种重要指标。以caspase-3为靶点设计凋亡靶向特异性探针,通过对其表达水平进行监测可以及时评估肿瘤疗效。本研究报道了一... 诱导肿瘤细胞凋亡是多种肿瘤治疗方案的作用机制之一,因此检测肿瘤细胞是否产生凋亡已成为评价肿瘤治疗疗效的一种重要指标。以caspase-3为靶点设计凋亡靶向特异性探针,通过对其表达水平进行监测可以及时评估肿瘤疗效。本研究报道了一种靶向caspase-3的正电子发射断层显像(PET)探针[^(18)F]8。采用简便的固相合成法和点击缩合法合成多肽和前体8,利用^(18)F-^(19)F氟离子交换法进行放射性核素氟-18标记,得到放射化学产率16%和放射化学纯度95%的探针[^(18)F]8。探针[^(18)F]8在PBS和小鼠血清中具有较好的稳定性,脂水分配系数Log P为-1.69±0.01,表明探针亲水性较好。高效的合成方法以及良好的理化性质为探针应用于肿瘤凋亡模型的PET成像研究奠定了良好的基础。 展开更多
关键词 肿瘤凋亡 CASPASE-3 分子探针 正电子发射断层显像 氟-18标记 合成 表征
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^(68)Ga标记四嗪探针^(68)Ga-NOTA-Tz的制备与体内外性质评价
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作者 张丰盛 王撵 +2 位作者 宋少莉 杨红 王明伟 《肿瘤影像学》 2023年第5期445-452,共8页
目的:探索一种^(68)Ga标记四嗪探针(^(68)Ga-NOTA-Tz)的优化标记条件,并评价其体内外性质。方法:开展^(68)GaNOTA-Tz的标记条件优化实验,包括反应体系的p H值、温度、时间和前体用量等4种影响因素。利用放射性快速薄层色谱(Radio-i TLC... 目的:探索一种^(68)Ga标记四嗪探针(^(68)Ga-NOTA-Tz)的优化标记条件,并评价其体内外性质。方法:开展^(68)GaNOTA-Tz的标记条件优化实验,包括反应体系的p H值、温度、时间和前体用量等4种影响因素。利用放射性快速薄层色谱(Radio-i TLC)和放射性高效液相色谱(Radio-HPLC)测定^(68)Ga-NOTA-Tz的标记率和体外稳定性,并进行脂水分配系数log P、血浆蛋白结合率、BALB/c正常鼠血液半衰期和生物分布、以及在SMMC-7721移植瘤模型Micro PET/CT显像等体内外性质评价。结果:根据优化实验结果,^(68)Ga-NOTA-Tz最佳标记条件是反应体系p H=3.8、反应温度45℃、反应时间10 min、前体用量5 nmol,在此条件下其标记率大于95%。体外实验显示,^(68)Ga-NOTA-Tz在生理盐水和胎牛血清中的稳定性分别保持在95%和90%以上(4 h内),其脂水分配系数log P为-2.06±0.02,血浆蛋白结合率为20%左右(1.5 h内)。血液半衰期实验表明,^(68)Ga-NOTA-Tz的早期快速分布半衰期为1.1 min、终末缓慢清除半衰期为29.1 min。体内生物分布和肿瘤Micro PET/CT发现,^(68)Ga-NOTA-Tz主要分布于肝、胆、肾脏和膀胱等代谢器官,对应的%ID/g均较高,同时在肿瘤组织均匀分布,0.5、1.0、1.5 h时的%ID/gmean分别为1.6±0.11、1.3±0.15和1.3±0.12,与肌肉和心脏的较为接近。结论:本研究优化建立了四嗪探针^(68)Ga-NOTA-Tz的制备条件,其标记率高,具有良好的稳定性和亲水性,在体内能快速而均匀地分布至肿瘤组织,有利于其应用于基于体内生物正交点击反应的肿瘤预靶向PET/CT显像。 展开更多
关键词 核素^(68)Ga 放射性标记 四嗪探针 正电子发射体层成像/计算机体层成像 肿瘤
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抗体介导偶联药物开发中的几个关键点
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作者 辛英豪 王丽丽 +3 位作者 李明洋 徐霖 于占娇 李元浩 《中国食品药品监管》 2023年第12期92-111,共20页
抗体偶联药物(ADC)和抗体介导的核素偶联药物(RDC)作为抗肿瘤靶向生物药,已经在过去的10年中引起了广泛的关注。本文介绍靶向药物的研发历程以及ADC概况,讨论ADC开发中的几个关键问题,如开发风险、临床毒性、内吞与药效以及结合位点屏... 抗体偶联药物(ADC)和抗体介导的核素偶联药物(RDC)作为抗肿瘤靶向生物药,已经在过去的10年中引起了广泛的关注。本文介绍靶向药物的研发历程以及ADC概况,讨论ADC开发中的几个关键问题,如开发风险、临床毒性、内吞与药效以及结合位点屏障作用的影响等,并分析ADC的延伸——抗体介导的RDC的开发进展和独特优势等,旨在通过分析与讨论ADC和RDC在临床上的应用前景和改进措施,为靶向生物药的发展提供创新方向。 展开更多
关键词 靶向药物 抗体偶联药物 核素偶联药物 关键风险 临床毒性 内吞与药效 结合位点屏障
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雾化吸入干扰素α1b在兔体内的分布及代谢途径 被引量:57
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作者 刘鉴峰 刘金剑 +3 位作者 褚丽萍 王德芝 于佳 刘金毅 《医药导报》 CAS 北大核心 2013年第1期1-5,共5页
目的研究雾化吸入与肌内注射干扰素α1b(IFNα1b)在兔体内分布及代谢的差异,考察雾化吸入干扰素治疗肺部疾病的优越性。方法将干扰素α1b进行125I标记,选用新西兰大耳白兔,以肌内注射为对照,采用雾化吸入的方式给药,不同时间点取血,γ... 目的研究雾化吸入与肌内注射干扰素α1b(IFNα1b)在兔体内分布及代谢的差异,考察雾化吸入干扰素治疗肺部疾病的优越性。方法将干扰素α1b进行125I标记,选用新西兰大耳白兔,以肌内注射为对照,采用雾化吸入的方式给药,不同时间点取血,γ计数仪测定血药浓度,通过小动物活体成像系统和γ计数仪检测肺组织不同部位的药物分布情况和主要代谢脏器肝和肾中的药物含量。结果与肌内注射比较,雾化吸入给药后肺组织中的干扰素含量更高,肺组织内滞留时间长,血药浓度达峰时间为8 h,明显延迟,而肾组织中的药物含量始终维持较低浓度。结论与常规肌内注射给药相比,雾化吸入干扰素α1b肺组织药物含量高,药物体内循环时间长,是干扰素治疗肺部疾病更为有效的给药途径。 展开更多
关键词 干扰素Α1B 雾化吸入 125I标记
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^(125)I-RC-160的标记方法研究及其正常小鼠体内的分布特征 被引量:6
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作者 汪静 王喜青 +2 位作者 王连刚 李富军 邓敬兰 《核技术》 CAS CSCD 北大核心 2002年第11期897-900,共4页
研究了一种高效碘标多肽RC - 16 0的方法 ,在其中以溴代琥珀酰亚胺 (NBS)为氧化剂 ,常规氯胺T法作为对照。对12 5I -RC - 16 0的标记率、比活度进行了评价 ,并观察12 5I -RC - 16 0在正常小鼠体内的生物分布特征。结果显示 :在丙酮:生... 研究了一种高效碘标多肽RC - 16 0的方法 ,在其中以溴代琥珀酰亚胺 (NBS)为氧化剂 ,常规氯胺T法作为对照。对12 5I -RC - 16 0的标记率、比活度进行了评价 ,并观察12 5I -RC - 16 0在正常小鼠体内的生物分布特征。结果显示 :在丙酮:生理盐水 =1:1体系中 ,测得12 5I -RC - 16 0的标记率NBS法为 92 %,比活度为 1.95× 10 12 Bq/mmoL ,标记率随NBS用量增加而增高 ,最佳用量比为RC - 16 0 (μg):12 5I(MBq):NBS(μg) =3:7.4:1,且产物无需纯化 ;Ch -T法标记率为5 6 %,比活度为 0 .6 5× 10 12 Bq/mmoL ,经SepPaK -C18反向色谱柱纯化 ,12 5I -RC - 16 0的标记率可达 92 %。标记物在血中清除较快 ,注射后不到 1h血中的放射性就下降了 87.2 %;12 5I -RC -16 0在甲状腺及肾的浓集度很低 ,主要经过消化系统排出体外。 展开更多
关键词 分布特征 生长抑素类似物 放射性同位素 同位素标记 碘125 代谢 RC-160
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新型除草剂丙酯草醚A环^(14)C均标记合成和鉴定 被引量:15
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作者 杨征敏 叶庆富 +2 位作者 唐庆红 吕龙 陈子元 《化学学报》 SCIE CAS CSCD 北大核心 2005年第21期1999-2003,共5页
以U-14C-对氨基苯甲酸为前体,通过酯化、缩合、还原和取代四步反应获得了A环14C均标记的丙酯草醚,用PHPLC对其进行纯化.采用HPLC-MS(ESI),MS(EI)和1HNMR验证了其结构,通过HPLC(外标法)确定其化学纯度大于98%;HPLC-LSC和TLC-IIA两种方法... 以U-14C-对氨基苯甲酸为前体,通过酯化、缩合、还原和取代四步反应获得了A环14C均标记的丙酯草醚,用PHPLC对其进行纯化.采用HPLC-MS(ESI),MS(EI)和1HNMR验证了其结构,通过HPLC(外标法)确定其化学纯度大于98%;HPLC-LSC和TLC-IIA两种方法分析表明,其放射化学纯度大于98%,其比活度为1.089±0.011mCi/mmol.合成的化学收率和放化收率均为53%. 展开更多
关键词 丙酯草醚(A-环-U-^14C) 放射性标记合成 鉴定 除草剂 ^14C 丙酯草醚 新型除草剂 合成 标记 A环
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^(99)Tc^m-DTPA-DG标记物的制备 被引量:7
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作者 陈跃 黄占文 +2 位作者 何菱 郑时龙 李举联 《核化学与放射化学》 EI CAS CSCD 北大核心 2006年第2期125-128,共4页
为了在合成二乙三胺五乙酸-脱氧葡萄糖(DTPA-DG)基础上,制备99Tcm-DTPA-DG标记物,以SnCl2.2H2O为还原剂,还原99TcmO4-并与DTPA-DG形成99Tcm-DTPA-DG标记物。进行了DTPA-DG用量、SnCl2.2H2O用量、反应介质pH值、反应温度等对标记率的影... 为了在合成二乙三胺五乙酸-脱氧葡萄糖(DTPA-DG)基础上,制备99Tcm-DTPA-DG标记物,以SnCl2.2H2O为还原剂,还原99TcmO4-并与DTPA-DG形成99Tcm-DTPA-DG标记物。进行了DTPA-DG用量、SnCl2.2H2O用量、反应介质pH值、反应温度等对标记率的影响实验。结果表明,25 mg DTPA-DG,500μg SnCl2.2H2O,pH=6,加入Na99TcmO4淋洗液0.5~4 mL,在25℃以上放置30 min或沸水浴反应10 min时,用9 g/LNaCl和丙酮作展开剂纸层析法鉴定标记物,放射化学纯度>99%。标记物在室温放置6 h,放射化学纯度仍达98.6%9。9Tcm-DTPA-DG标记率高,标记物的体外稳定性好,操作简便,便于临床应用。 展开更多
关键词 DTPA-DG ^99Tc^m-DTPA-DG ^99Tc^mO4^- 放射性核素标记
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^(99)Tc^m标记的小干扰RNA探针的制备及稳定性评价 被引量:5
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作者 康磊 王荣福 +5 位作者 闫平 刘萌 张春丽 于明明 崔永刚 徐小洁 《核化学与放射化学》 CAS CSCD 北大核心 2010年第6期348-353,共6页
通过偶联双功能螯合剂S-乙酰基-MAG3以达到制备99Tcm标记的小干扰RNA探针的目的,并对其标记条件及体外稳定性进行评价。结果表明,室温下99Tcm-siRNA在反应时间大于1 h、SnCl2.2H2O质量浓度小于2 g/L时,标记率可达(73.4±3.0)%;经Sep... 通过偶联双功能螯合剂S-乙酰基-MAG3以达到制备99Tcm标记的小干扰RNA探针的目的,并对其标记条件及体外稳定性进行评价。结果表明,室温下99Tcm-siRNA在反应时间大于1 h、SnCl2.2H2O质量浓度小于2 g/L时,标记率可达(73.4±3.0)%;经Sephadex G25纯化后其放化纯度大于92%,比活度达25.9 PBq/mol;在室温和37℃条件下,99Tcm-siRNA于生理盐水和血清中均保持良好的标记稳定性;标记后的siRNA探针与未标记探针具备相似的靶向干扰活性。 展开更多
关键词 小干扰RNA 99Tcm 标记 稳定性
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^(99)Tc^m标记的annexinV检测不稳定动脉粥样硬化斑块的实验研究 被引量:5
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作者 赵全明 许金鹏 +2 位作者 王蒨 陈大明 米洪志 《中国医学影像技术》 CSCD 北大核心 2005年第9期1349-1352,共4页
目的探讨放射标记的膜联蛋白无创检测不稳定斑块的可行性。方法6只新西兰大白兔随机分为实验组和对照组。实验组3只白兔通过球囊拉伤膈下降主动脉内膜,并饲喂含2%胆固醇的高脂饲料15周,制造动脉粥样硬化模型;对照组仅饲喂普通饮食。实验... 目的探讨放射标记的膜联蛋白无创检测不稳定斑块的可行性。方法6只新西兰大白兔随机分为实验组和对照组。实验组3只白兔通过球囊拉伤膈下降主动脉内膜,并饲喂含2%胆固醇的高脂饲料15周,制造动脉粥样硬化模型;对照组仅饲喂普通饮食。实验组3只家兔分别注射99TcmannexinⅤ20μg、200μg和500μg,降主动脉活体核素成像和离体核素成像,以及动脉标本数码照相。实验组降主动脉分段,测定其放射强度。结果注射500μg99TcmannexinⅤ5min和120min后,实验性动脉粥样硬化动物沿腹主动脉走行即可见一条放射性浓集的条状影像。离体降主动脉核素成像与大体标本数码照相病变斑块相一致。粥样硬化斑块明显的节段,靶非靶比值也相对较高。结论99TcmannexinⅤ核素成像检测实验性动脉粥样斑块具有一定的可行性,可发展成为一种无创检测不稳定斑块的方法。 展开更多
关键词 不稳定斑块 放射标记的膜联蛋白
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