Radioiodine-Labeling of Chlorpyrifos and Its Biodistribution in Mice

To investigate the preparation of radioiodinated Chlorpyrifos and its biodistribution in mice, Chlorpyrifos was labeled with¹³¹I using the Iodogen method. Biodistribution studies were carried out in KM mice. At different times after radiopharmaceutical i.v. administration (185 kBq¹³¹I-Chlorpyrifos/mouse, n=5), the animals were sacrificed. Blood samples and the tissues of interested were collected, weighted and counted. The percentage of injected does per gram (%ID/g) was calculated for each sample. The labeling yield of ¹³¹I-Chlorpyrifos was 93.5%, The radiochemical purity (RCP) was 96.9%. Biodistribution in mice demonstrated that¹³¹I-Chlorpyrifos was extensive, and the uptakes mainly occur in lung, stomach, small-intestine, colon, musle, and submaxillay gland, as indicated by their amount of 37.12%ID/g, 6.18%ID/g, 8.12%ID/g, 8.15%ID/g, 7.04%ID/g, and 7.02%ID/g at 10 min, respectively. And it was metabolized in liver and kidney, as indicated by their uptake of 4.34%ID/g and 8.50%ID/g at 5 min, and 0.22%ID/g and 0.69%ID/g at 4 h, respectively. In addition,¹³¹I-Chlorpyrifos was cleared out from blood quickly, and the uptake of¹³¹I-Chlorpyrifos in blood was 37.27%ID/g at 5 min, and decreased to 1.35%ID/g at 4 h post injection. In conclusion, ¹³¹I-Chlorpyrifos was stable in vitro and it was absorbed in lung and digestive tract, and it was metabolized mainly in liver and kidney, worthy of further investigation to trace the compound in vivo and in vitro.     

碘标记毒死蜱及其在小鼠体内的生物分布

为探讨¹³¹I标记毒死蜱（Chlorpyrifos, CPF）在小鼠体内的分布特点,采用Iodogen法对CPF进行¹³¹I标记,KM小鼠尾静脉注射¹³¹I-CPF（185 kBq/只,n=5）,分别于注射后5、10、30、60、120、240、1440 min取各脏器,计算每克组织摄取注射剂量的百分率（%ID/g）。结果显示,¹³¹I-CPF标记率达93.5%,放化纯度为96.9%,¹³¹I-CPF在小鼠体内广泛分布,主要经肺、胃、小肠、大肠、肌肉和颌下腺吸收,其放射性摄取率在注药后 10 min 时达高峰,分别为37.12%ID/g、6.18%ID/g、8.12%ID/g、8.15%ID/g、7.04%ID/g和7.02%ID/g;经肝和肾进行代谢,其放射性摄取率在5 min时分别为4.34%ID/g和8.50%ID/g, 4 h为0.22%ID/g和 0.69%ID/g。血液中放射性清除较快,放射性摄取率在注入后5 min时为37.27%ID/g,4 h为1.35%ID/g。碘标记CPF体外稳定,体内主要经肺和消化道吸收,肝、肾代谢,可用于进一步的微量示踪研究。     

Radioiodine labeled SP-4 as an imaging agent foratherosclerotic plaques

1 INTRODUCTIONAtherosclerosis is the major cause of death on the world. Current jlnaging techniquesfor adaging atherosclerosis, such as angiography, ultrasound, computed tomography andnuclear magnetic resonance, are good at defting the extent of more advanced atherosclerotic plaques, but cannot detect the formation of atherosclero,is[1]. If we can find out anew method that can detect atherosclerosis in progress, then we may change the dietaryof patient, use drug or other means to hold back…     

125I标记的羊抗人IgG多克隆抗体在荷人结肠癌裸鼠体内的生物分布及γ显像

采用Iodogen法对羊抗人IgG多克隆抗体(GAHG)进行125I标记,评价其体外稳定性及药代动力学性质,观察125I-GAHG在荷HT-29人结肠癌裸鼠中的生物分布和γ显像,探讨肿瘤细胞分泌的IgG作为靶点进行肿瘤放射免疫显像和治疗的可能性。结果显示,125I-GAHG具有良好的体外稳定性,其血液清除符合二室模型,T1/2α和T1/2β分别为1.19 h和43.99 h。尾静脉给药后,与125I标记的正常羊IgG(125I-GIgG)对照相比,125I-GAHG具有更加明显的肿瘤摄取。瘤体内给药显示125I-GAHG在肿瘤部位具有良好的滞留。在静脉注射后72 h,肿瘤摄取达到最大,为6.71 ± 2.19 %ID/g。靶组织与非靶肿瘤放射性比值(T/NT)随着时间延长逐渐增高。上述结果表明,肿瘤分泌的IgG为肿瘤放射免疫显像和靶向治疗提供了新的靶点和研究思路。     

^59Fe示踪法测定纳米级磁性氧化铁在小鼠体内的分布

将     

红景天苷的碘标记及其在小鼠体内的分布

通过131碘标记红景天苷以探索红景天苷在神经母细胞(SH-SY5Y)中的摄取及在小鼠体内的代谢分布.采用氯胺-T法对红景天苷进行131碘标记;以聚酰胺薄膜为支持介质、V三氯甲烷:V甲醇:V丙酮:V水=6:3:1:1的下层液为展开剂,测定标记率及标记物放化纯;分析神经母细胞SH-SY5Y及肿瘤细胞MCF-7对131I-红景天苷的摄取;KM小鼠尾静脉注射131I-红景天苷(1.85 MBq/只,n=5),于5、10、30、60、120、240 min分别取心、肝、肺、肾、脾、肌、骨、脑、肠、血,称重、计数,计算每克组织百分注射剂量率(%ID/g).结果表明,131I-红景天苷标记率达98%,其放化纯在1、4、20 d分别为98.5%、97.3%、97.1%;SH-SY5Y对131I-红景天苷基本无摄取,在0.5-4 h内摄取维持在0.035%左右,而MCF-7则为0.1%;131I-红景天苷在体内主要通过肝代谢、肾排泄,其中肝和肾5 min%ID/g组织分别为7.71%和11.32%,4 h则分别下降为0.36%和0.3%;血液中清除也较快,5 min时为6.41%,4 h为0.35%;在脑中虽分布较少,但清除较慢,5 min时为0.27%,4 h为0.11%;在心、肺、脾、肌、骨及肠中分布不多.结论是,碘标红景天苷标记率高,标记物稳定;神经母细胞对131I-红景天苷基本无摄取.     

99Tcm标记NGR及其在荷人HePG2肝癌裸鼠体内的生物分布及SPECT显像

用⁹⁹Tc^m标记了含有天冬酰胺-甘氨酸-精氨酸（Asn-Gly-Arg）序列的血管靶向性短肽NGR,评价了标记物⁹⁹Tc^m-NGR的放化性质以及在荷HePG2肝癌模型裸鼠体内的生物分布和SPECT显像。标记结果显示,⁹⁹Tc^m-NGR的标记率>90%,放化纯度>95%。荷瘤裸鼠体内生物分布结果显示,⁹⁹Tc^m-NGR在肾脏和肝脏的摄取率较高,注射后1 h肿瘤摄取达（2.52±0.62）%ID/g,最高达（7.26±2.71）%ID/g,12 h仍然达（3.93±1.93）%ID/g,但在竞争性抑制组中摄取率为（1.29±0.85）%ID/g。荷瘤裸鼠的SPECT显像结果显示,除肿瘤外,其他组织器官的放射性摄取随时间延长逐渐降低,肿瘤与肌肉组织的放射性攝取比（T/NT）4 h时最高,可达3.25。注射后1 h肿瘤可见,12 h时最为清晰。以上结果提示,⁹⁹Tc^m-NGR易于制备,具有良好的靶向性, 在肿瘤的诊疗中具有良好的研究前景。     

64Cu-NOTA-NOC的制备及体内生物分布初步研究

对生长抑素八肽类似物NOTA-NOC进行⁶⁴Cu标记,并对⁶⁴Cu-NOTA-NOC的体外稳定性、脂水分配系数、正常及荷瘤小鼠体内分布进行初步研究。建立⁶⁴Cu-NOTA-NOC的标记及质控条件;考察⁶⁴Cu-NOTA-NOC的体外稳定性,测定其脂水分配系数;通过尾静脉注射⁶⁴Cu-NOTA-NOC至小鼠体内,进行生物分布研究。结果表明：室温条件下即可获得标记率大于95%的⁶⁴Cu-NOTA-NOC;⁶⁴Cu-NOTA-NOC在缓冲溶液及10%胎牛血清溶液中具有良好的稳定性,脂水分配系数为-1.12±0.005 6;⁶⁴Cu-NOTA-NOC在正常昆明（KM）小鼠体内主要经肾脏代谢,血液摄取值随时间下降明显,显示其体内清除速度较快;在荷BON-1胰腺癌裸鼠体内也主要经肾脏代谢;在肿瘤中具有较高的摄取,注后2 h,肿瘤/肌肉摄取比值达10.38;荷BON-1胰腺癌裸鼠的PET/CT显像结果显示,1 h时,肿瘤对⁶⁴Cu-NOTA-NOC的摄取率最高,为7.7%ID/g,而给予阻断剂后,肿瘤对⁶⁴Cu-NOTA-NOC的摄取率显著降低,为0.94%ID/g。NOTA-NOC的⁶⁴Cu标记在室温条件下即可完成,⁶⁴Cu-NOTA-NOC在缓冲溶液及10%胎牛血清中具有较好的稳定性;其在动物体内主要经肾脏代谢,体内清除较快,在胰腺癌肿瘤组织中有较高摄取;PET/CT实验结果显示肿瘤对⁶⁴Cu-NOTA-NOC的摄取具有特异性。初步的研究结果表明,⁶⁴Cu-NOTA-NOC具有用于胰腺癌诊疗的潜质,值得开展进一步研究。     

18F标记哒嗪酮类似物的制备及其在小鼠体内的生物分布

设计并合成了一种18F标记哒嗪酮类似物：2-特丁基-4-氯-5-(2 氟[18F]乙氧基)-2H-3-哒嗪酮（18F-FP2）,通过生物分布实验评价了其用于心肌灌注显像的可行性。18F-FP2的总制备时间为70～90 min,校正后的放化产率为53.0%±5.2%,放化纯度>98%;18F-FP2为脂溶性化合物,在水溶液中可稳定放置3 h以上。生物分布实验结果显示,18F-FP2在肝、肺中初期摄取高,注射后2 min分别为（14.53±2.36）%ID/g和（33.69±10.79）%ID/g,但清除很快,注射后15 min,其肝、肺的清除率已分别达57.7%和86.2%。18F-FP2的心肌摄取较低,最高摄取值为（4.09±0.53）%ID/g（注射后2 min）。这可能因标记侧链上未带苯环造成的,说明哒嗪酮侧链的芳环结构对心肌的摄取与滞留有较大影响。     

Biodistribution and pharmacokinetics of ^99mTc—CQDO and ^99mTc—CQDO—MeB for new myocardial imaging agent

A comparison of ~(99m)Tc- CQDO and ~(99m)Tc-CQDO-MeB has been made for biodistribution and pharmacokinetics. ~(99m)Tc-CQDO and its adducts of methaneboronic acid ~(99m)Tc-CQDO-MeB were prepared by the reduction of Na~(99m)TcO_4 with SnCl_2·2H_2O in aqueous solution. Radiochemical purity of ~(99m)Tc-CQDO and ~(99m)Tc-CQDO-MeB determined by TLC were over 95% after extraction. Biodistributions of ~(99m)Tc-CQDO and ~(99m)Tc-CQDO-MeB in mice demonstrated that both of them could be easily absorbed by myocardium, and the peak uptake of each were 10.83±2.2% ID/g and 11.84±1.69%ID/g, respectively. ~(99m)Tc-CQDO showed rapid clearance from myocardial tissue while ~(99m)Tc-CQDO-MeB had long retention in heart muscle. The myocardial uptake of ~(99m)Tc-CQDO was only 5.88±1.66%ID/g at 10 min. and the uptake of ~(99m)Tc-CQDO-MeB was 7.42±0.17%ID/g at 60 min. The elimination of each from blood has a biexponential pattern, the first T_(1/2) is 1.38 and 1.5 min, respectively. The partition coefficient of ~(99m)Tc-CQD     

Preparation and biodistribution of ^99Tc^m-PIDP as bone imaging agent

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 SnCI2.2H2Cl2·2H2O 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.     

125I标价重组MIF在炎症模型小鼠体内的生物分布

摘要：目的:初步评价125I标记巨噬细胞移动抑制因子（MIF）在炎症显像中的应用价值。方法：Iodogen法制备125I-MIF,研究其稳定性、特异性及在炎症模型小鼠体内的生物学分布规律。结果：125I-MIF的标记率为96.5%,室温下48小时内标记化合物的生物学性质稳定。体内分布表明125I-MIF主要由肝脏代谢,经肾脏排泄,血液清除较快。尾静脉注射125I-MIF 0.5、1、6、24小时后,炎症肢体（靶）与对侧健肢（非靶）的%ID比值（T/NT）值分别为1.42、1.35、2.18和2.05。结论：125I-MIF具有在活体内炎症定位导向能力,但在早期优越性不明显,6小时后效果较佳,对隐匿性或亚急性炎症病灶的诊断有潜在的临床价值。     

Preparation and preliminary biological evaluation of 99Tcm-TADP as bone imaging agent

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. 99Tcm-TADP was prepared with 5 mg TADP at Ph 7.0 by joining 99TcmO4 with SnCl2·2H2O in aqueous solution for 10 min at room temperature. Both labeling yield and radiochemical purity of 99Tcm-TADP were more than 95%. The biodistribution in rats and bone scan in rabbits were also studied. The 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 99Tcm-TADP in rats, bone-to-muscle and bone-to-blood uptake 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.     

Preparation and bio-distribution of bone tumor therapeutic agent 188Re-TCTMP

1 Introduction Several radionuclides, such as 153Sm, 186Re, 177Lu,212Bi, 211At and 117mSn, have been used for bony me-tastases.[1-7] But the nuclides mentioned above areusually difficult to prepare in spite of their excellentphysical and chemical characteristics. Recently, 188Rehas been focused because of its excellent nuclearcharacteristic and easy availability.[8-10] The mecha-nism of bone uptake of 99m Tc-diphosphonates wasbelieved to be related to…     

[99TcmN(PNP)]2+标记葡萄糖硫酮类衍生物混配配合物的研究

为研究新的99TcmN核心标记的心肌和肿瘤显像药物,选用自行合成的二硫化碳-葡萄糖(硫酮类)衍生物Ln(L1～L5)制备一系列带有葡萄糖衍生物基团的新型[99Tcm (DTC)(PNP)]+类配合物,经TLC和HPLC检测,配合物的放射化学纯度均大于90%.小鼠生物分布实验表明,99TcmN(PNP)Ln(L1～L5)系列配合物在正常小鼠体内初始的放射性摄取主要分布于心肌、肝、肺、肾等脏器,并且30 min内各脏器均可迅速清除.初步的荷EMT-6鼠生物分布实验显示,99TcmN(PNP)L2在肿瘤中放射性摄取不高,30 min时为(0.39±0.03)%ID/g,其它组织的放射性摄取与正常小鼠类似.     

~(125)I-OxLDL-Ab在正常小鼠及动脉粥样硬化动物模型体内的生物分布

分别采用高效液相色谱法、紫外分光光度法对OxLDL-Ab进行定性、定量分析,评价~(125)I-OxLDL-Ab在正常动物和动脉粥样硬化模型动物的体内分布。正常动物采用昆明小鼠,模型采用载脂蛋白E基因敲除的小鼠(apolipoprotein E-deficient mice,ApoE~(-/-))。高效液相色谱条件为:磷酸缓冲液(PB,0.2 mol/L,pH=7.4)为流动相,流速1.0mL/min,检测波长220nm;紫外分光光度法测得蛋白浓度的标准曲线为:y=0.664 5x-0.008 3,r2=0.999 7。~(125)I-OxLDL-Ab在正常小鼠体内分布实验结果表明:除甲状腺外,各器官的放射性摄取随时间延长而减少,无明显浓集;在注射~(125)I-OxLDL-Ab后1d各器官代谢消除超过2/3,7d后血液中完全清除。~(125)I-OxLDL-Ab在ApoE~(-/-)鼠体内的分布实验中采用w=2%的KI溶液封闭了甲状腺,消除了甲状腺高摄取的影响;靶器官肺有较高放射性摄取,且在注射后4~8h显示出放射性浓集;除血外,其它各器官的靶器官/非靶器官的放射性摄取比值(T/NT)均大于1,其中T/Mu(肌肉)8,显示出~(125)I-OxLDL-Ab对靶器官有一定的选择性。标记抗体的体内靶向性是显像研究中至关重要的一环,要进一步用于动脉粥样硬化早期显像诊断,还需进一步提高靶器官/非靶器官的放射性摄取比值,提高其在体内与其抗原的亲和性。     

新型Aβ斑块显像剂18F-W372

合成诊断阿尔茨海默病（Alzheimer’s disease,AD）的Aβ斑块显像剂：7-甲氧基-2(6-［¹⁸F］-氟-吡啶-3-基)咪唑［2,1-β］-8-吡啶噻唑（¹⁸F-W372）,不校正合成效率为（25.3±7.1）%（n=6）,产品放化纯大于99.5%,比活度为659~721PBq/mol。 ^{18F-W372小鼠体内分布实验显示,初始5min脑摄取为（4.36±1.44）%ID/g,清除较快,30min为（0.54±0.16）%ID/g,摄取比达到8,具有良好的生物学性能。急性毒性实验表明该药物安全可靠。在体试验显示药物注射40min,AD患者平均皮层/小脑吸收显著高于健康老年对照组。18F-W372是一种潜在的脑内Aβ淀粉显像剂。}     

NGR短肽的188Re标记及其在荷瘤裸鼠体内的生物分布和SPECT显像

采用¹⁸⁸Re标记含有天冬酰胺、甘氨酸、精氨酸（Asn-Gly-Arg,NGR）序列的肿瘤血管靶向性短肽,得到¹⁸⁸Re-NGR,观察了¹⁸⁸Re-NGR在荷HepG2肝癌细胞严重联合免疫缺陷（Severe Combined Immunodeficiency,SCID）裸鼠肿瘤模型中的生物分布,并对其进行了SPECT显像。结果显示,¹⁸⁸Re-NGR的标记率>85%,放化纯度>90%。¹⁸⁸Re-NGR在肿瘤模型鼠体内的生物分布显示,注射¹⁸⁸Re-NGR后12 h,肿瘤放射性摄取达最高,为(4.62±0.71)%ID/g,24 h时仍有(2.01±0.38)%ID/g,说明标记物在肿瘤内停留时间较长;竞争性抑制组中,12 h肿瘤放射性摄取为(1.43±0.61)%ID/g,明显低于实验组。肿瘤与肌肉组织的放射性摄取比(T/NT) 12 h为4.76。注射后1 h肿瘤可显像,4～8 h显像逐渐清晰,12 h时更为清晰。以上结果提示,¹⁸⁸Re-NGR具有良好的肿瘤血管靶向性。     

The Research onBiodistribution of 131I-Iodosennoside A in Normal Mice and toEvaluate Myocardial Activity

Purpose: The objective ofthis project is to evaluate biodistribution of [¹³¹I]Iodosennoside Ain normal mice and explore the feasibility on the diagnosis of myocardialinfarction. Methods: Iodogen method was used to radioiodinate sennoside A with¹³¹I.[¹³¹I]Iodosennoside A was intravenously injected into mice. Threegroups of mice were killed at 4 h, 24 h and 48 h post injection respectivelyand the radioactive uptake in major organs were calculated. Rats were subjectedto left anterior descending (LAD) coronary artery ligation to induce acutemyocardial infarction. Rat models of myocardial infarction were intravenouslyinjected [¹³¹I]iodosennoside A. 24 h after injection of [¹³¹I]iodosennosideA, the regional distribution of radioiodinated sennoside A was determined byradioactivity counting technique. 2,3,5-triphenyl tetrazolium chloride (TTC)staining and autoradiography were performed with 2 mm thick sections of heartsfor postmortem verifications. Results: The study showed high uptake of [¹³¹I]iodosennosideA in kidneys and fast blood clearance. At 24 h post injection, radioactivityconcentration in infarcted myocardium was over 11.9 times higher than in normalmyocardium. Preferential uptake of the [¹³¹I]iodosennoside A innecrotic tissue was confirmed by perfect match of images from TTC staining andautoradiography. Conclusion: The result proved that [¹³¹I]iodosennosideA has myocardial necrosis affinity and may serve as a marker on the diagnosisof myocardial infarction.