肿瘤阳性显像剂5-18F-fluorouracil的标记与动物实验

目的 探讨^18F-fluorouracil（FU）作为肿瘤阳性显像剂的可能性。方法 标记与合成了^18F-FU,研究其在正常与荷瘤裸鼠中的生物分布,进行正常与荷瘤兔的PET显像。HPLC及其他质控分析结果均证实^18F-FU动物实验与临床应用的可行性,生物分布及显像研究表明它在肿瘤组织中有较多的摄取。结论 ^18F-FU是一种有潜力的肿瘤阳性显像剂。     

99Tcm-DTPA-DG的制备及其荷瘤裸鼠实验研究

目的进行99Tcm-DTPA-脱氧葡萄糖(DG)的化学合成、标记物制备、质量控制及药理研究.方法合成的DTPA-DG用氯化亚锡作还原剂,与99TcmO4-混合,在25℃以上室温放置30 min或沸水浴反应10nin,用一步法进行99Tcm标记.丙酮和质量分数0.9%生理盐水作展开剂,用纸层析法鉴定99Tcm-DTPA-DG的放化纯、标记稳定性;进行乳腺癌MCF-7裸鼠体内生物分布实验及显像研究.结果标记产物放化纯＞99%.99Tcm-DTPA-DG荷瘤裸鼠生物分布显示,肿瘤/血液比值1、2 h分别为1.29、3.13,肿瘤/肌肉比值1、2 h分别为2.63、5.01.荷瘤裸鼠99Tcm-DTPA-DG显像显示肿瘤组织.结论99Tcm-DTPA-DG可能成为肿瘤葡萄糖代谢显像剂.     

乏氧组织显像剂^99Tc^m—DTPA—甲硝唑的制备和荷瘤动物实验研究

目的　进行新型乏氧组织显像剂DTPA-甲硝唑的化学合成、药盒制备、99Tcm标记、质量控制以及药理研究。方法　合成的DTPA-甲硝唑用氯化亚锡作还原剂,99Tcm标记,用多元正交法确立99Tcm标记一步法药盒的最佳配方。纸层析法鉴定99Tcm-DTPA-甲硝唑的标记率、标记稳定性,完成了H22肝癌小鼠体内生物分布实验及显像研究。结果　DTPA-甲硝唑一步法药盒与99TcmO-4混合,沸水浴反应10min,放化纯度大于99%。H22肝癌小鼠生物分布显示,肿瘤/血液比值1、2h分别为3.43、6.40,肿瘤/肌肉比值1、2h分别为5.24、7.42;注射血管舒张药肼苯哒嗪组肿瘤组织摄取明显高于对照组（P<0.01）。结论　研制的99Tcm-DTPA-甲硝唑有望成为一种新型的肿瘤乏氧组织显像剂。     

O—（2—^18F—氟代乙基）—L—酪氨酸的合成及初步动物实验

目的 研制了^18F标记的氨基酸类肿瘤显像剂O-(2-^18F-氟代乙基）－L－酪氨酸（^18F-FET)。方法 亲核氟代法制备2－^18F-氟代乙醇对甲苯磺酸酯，再与酪氨酸二钠反应得^18F-FET。进行了小鼠体内分布实验和小鼠肿瘤显像。结果 ^18-FET放化收率4．4％，放化纯度＞99％。注射后60min小鼠肿瘤显像清晰，结论 ^18F-FET标记简便，小中瘤显像清晰。     

正电子肿瘤阳性显像剂^18F—AMT

^18F-AMT(^18F-α-methyl-tyrosine,^18F-α-甲基酪氨酸）是新研制的一种正电子肿瘤阳性显像剂。^18F-AMT的合成方法较简单，在肿瘤／非靶组织的比值高于^18F-FDG(^18F-氟代脱氧葡萄糖），特别是在脑肿瘤显像方面较^18F-FDG显示更大的优越性。     

生长抑素受体显像剂 99Tcm-HTOC的制备

目的　研制99Tcm 标记的生长抑素受体 (SSTR)阳性肿瘤显像剂99Tcm 6 肼基烟酰基 [Tyr3] octreotide (HTOC)。方法　通过四步化学反应合成 ,HPLC纯化 ,得到HTOC ;用乙二胺 N ,N′ 二乙酸 (EDDA)作为配体进行99Tcm 标记 ,测定标记率与标记物稳定性。结果　所合成HTOC质谱的分子离子峰与HTOC相对分子质量一致 ,99Tcm HTOC标记率 >95 % ,标记后 6h放化纯仍 >95 %。结论该法研制的99Tcm HTOC标记率高 ,体外稳定性好。     

FDG模块自动化合成2-18F-乙酸盐及其临床前研究

目的研究国产商用^18F—FDG模块自动化合成2-^18F-乙酸盐的可行性及其肿瘤显像。方法在商用FDG模块上未经修改参数，采用柱色层水解和纯化合成2-^18F-乙酸盐，并进行了放化纯、稳定性检测，生物学分布实验及荷乳腺癌和肺腺癌小鼠显像。结果采用商用FDG模块自动化合成2-^18F-乙酸盐，无需高效液相色谱（HPLC）法纯化，时间短，产率高，平均合成效率达59．3％，放化纯〉99％，合成时间为23min。2-^18F-乙酸盐的稳定性高，毒性较低，正常鼠生物学分布示血液清除慢，PET显像示乳腺癌和肺腺癌特异性摄取示踪剂。结论2^18F-乙酸盐是一种有潜在应用前景的肿瘤显像剂。     

自动化合成18F-FDDNP及其生物学分布

目的研究高效、简单的自动化合成脑内老年斑沉积显像剂2-(1-{6-[2-18F-乙基](甲基)氨}-2-萘-乙叉)丙二腈(18F-FDDNP)的方法及其小鼠生物学分布.方法采用化学过程控制单元(CPCU)控制整个过程,18F-在乙腈溶液中与前体2-(1-{6-[2-p-甲苯磺酰氧乙基](甲基)氨}-2-萘-乙叉)丙二腈直接反应生成18F-FDDNP,混合物装柱,产品被C-18柱吸附,用水冲洗柱,用少量乙醇淋出,加水稀释.NH小鼠给药后不同时间处死,分别取不同器官称重并测放射性计数.结果18F-FDDNP放化产率为35.7%(不校正),合成时间为20min,无需HPLC分离,放化纯＞95%.注射18F-FDDNP后,放射性主要分布在肝内,脑摄取较高,但清除较慢.结论自动化合成18F-FDDNP速度快,效率高.     

多巴胺转运蛋白显像剂18F-β-FP-CIT的合成与质量控制

目的研制多巴胺转运蛋白显像剂18F-N-3-氟丙基-2-β-甲酯基-3-β-(4-碘苯基)降托烷(18F-β-FP-CIT).方法 18F-β-FP-CIT经两步法制备1,3-二溴丙烷在相转移催化剂氨基聚醚钾复合物(K/K222)+18F-存在下发生亲核氟化反应,生成18F-氟丙基溴,后者与前体2β-甲酯基-3β-(4-碘苯基)降托烷 (nor-β-CIT)反应生成18F-β-FP-CIT.测定18F-β-FP-CIT主要质量控制指标.结果 18F-β-FP-CIT平均总放化产率约为8%,总放化合成时间约为90～110 min,放射化学纯度大于99%,其他主要质量控制指标达到放射性药物质量要求.结论合成的18F-β-FP-CIT注射液可用于动物和人体PET研究.     

利用Explora FDG4模块进行18F-氟乙酸盐自动化合成

目的 建立半衰期较长的18F-氟乙酸盐(FAC)的制备方法.方法 基于Siemens公司的Explora FDG4合成模块,增加3个试剂位和2个电磁阀,改编运行程序,以"两锅法"结合Sep-Pak简易分离柱的使用,完成18F-FAC的自动化合成.对荷W256肝癌大鼠行18F-FAC PET/CT显像.结果 该法合成时间为65 min,化学收率60%(时间校正),产品放化纯>98%.荷瘤大鼠PET显像示,30和120 min肿瘤标准摄取值(SUV)分别为1.37和1.20,肿瘤/前肢肌肉放射性比值分别为2.32和2.55.结论 用改进的Explora FDG4合成模块可以成功制备放化纯较高的18F-FAC.18F-FAC是一种有潜在应用价值的肝癌显像剂.     

PET imaging of colorectal cancer in xenograft-bearing mice by use of an 18F-labeled T84.66 anti-carcinoembryonic antigen diabody.

In this study, we investigated the 18F-labeled anti-carcinoembryonic antigen (CEA) T84.66 diabody, a genetically engineered noncovalent dimer of single-chain variable fragments, for small-animal PET imaging of CEA expression in xenograft-bearing mice. METHODS: 18F labeling of the anti-CEA T84.66 diabody (molecular mass, 55 kDa) was achieved with N-succinimidyl-4-18F-fluorobenzoate (18F-SFB). The biodistribution of the 18F-fluorobenzyl-T84.66 diabody (18F-FB-T84.66 diabody) was evaluated in athymic nude mice bearing subcutaneous LS 174T human colon carcinoma and C6 rat glioma tumors. Serial small-animal PET imaging studies were performed to further evaluate in vivo targeting efficacy and pharmacokinetics. RESULTS: Radiolabeling required 35 +/- 5 (mean +/- SD) min starting from 18F-SFB, and the tracer 18F-FB-T84.66 diabody was synthesized with a specific activity of 1.83 +/- 1.71 TBq/mmol. The decay-corrected radiochemical yield was 1.40% +/- 0.16% (n = 4), and the radiochemical purity was greater than 98%. The radioimmunoreactivity was 57.1% +/- 2.0%. The 18F-FB-T84.66 diabody showed rapid and high tumor uptake and fast clearance from the circulation in the LS 174T xenograft model, as evidenced by both small-animal PET imaging and biodistribution studies. High-contrast small-animal PET images were obtained as early as 1 h after injection of the 18F-FB-T84.66 diabody, and only a background level of activity accumulation was found in CEA-negative C6 tumors. The tracer exhibited predominantly renal clearance, with some activity in the liver and spleen at early time points. CONCLUSION: The 18F-labeled diabody represents a new class of tumor-specific probes for PET that are based on targeting cell surface antigen expression. The 18F-FB-T84.66 diabody can be used for high-contrast small-animal PET imaging of CEA-positive tumor xenografts. It may be translated to the clinic for PET of CEA-positive malignancies.     

Development of (18)F-fluoroethylcholine for cancer imaging with PET: synthesis, biochemistry, and prostate cancer imaging.

The effectiveness of (11)C-choline PET in detecting various cancers, including prostate cancer, is well established. This study was aimed at developing an (18)F-substituted choline analog, (18)F-fluoroethylcholine (FECh), as a tracer of cancer detection. METHODS: No-carrier-added (18)F-FECh was synthesized by 2-step reactions: First, tetrabutylammonium (TBA) (18)F-fluoride was reacted with 1,2-bis(tosyloxy)ethane to yield 2-(18)F-fluoroethyl tosylate; and second, 2-(18)F-fluoroethyl tosylate was reacted with N,N-dimethylethanolamine to yield (18)F-FECh, which was then purified by chromatography. An automated apparatus was constructed for preparation of the (18)F-FECh injection solution. In vitro experiments were performed to examine the uptake of (18)F-FECh in Ehrlich ascites tumor cells, and the metabolites were analyzed by solvent extraction followed by various kinds of chromatography. Clinical studies of (18)F-FECh PET were performed on patients with untreated primary prostate cancer as follows: A dynamic (18)F-FECh PET study was performed on 1 patient and static PET studies were performed on 16 patients, and the data were compared with those of (11)C-choline PET on the same patients. RESULTS: (18)F-FECh was prepared in high yield and purity. The performance of the automated apparatus was excellent. The in vitro experiment revealed that (18)F-FECh was incorporated into tumor cells by active transport, then phosphorylated (yielding phosphoryl-(18)F-FECh) in the cells, and finally integrated into phospholipids. The clinical PET studies showed marked uptake of (18)F-FECh in prostate cancer. A dynamic PET study on 1 patient revealed that the blood level of (18)F-FECh decreased rapidly (in 1 min), the prostate cancer level became almost maximal in a short period (1.5 min) and it remained constant for a long time (60 min), and the urinary radioactivity became prominent after a short time lag (5 min). Static PET studies conducted under bladder irrigation showed no difference between (18)F-FECh uptake and (11)C-choline uptake in prostate cancer. However, (18)F-FECh gave a slightly higher spatial resolution of the image, which was attributed to the shorter positron range of (18)F. CONCLUSION: The synthesis of (18)F-FECh was easy and reliable. (18)F-FECh PET was very effective in detecting prostate cancer in patients. The chemical trap, consisting of active transport of (18)F-FECh and formation of phosphoryl-(18)F-FECh, seemed to be involved in the uptake mechanism of (18)F-FECh in tumors.     

Evaluation of F-18-labeled amino acid derivatives and [18F]FDG as PET probes in a brain tumor-bearing animal model

2-Deoxy-2-[(18)F]fluoro-d-glucose ([(18)F]FDG) has been extensively used as positron emission tomography (PET) tracer in clinical tumor imaging. This study compared the pharmacokinetics of two (18)F-labeled amino acid derivatives, O-2-[(18)F]fluoroethyl-l-tyrosine (l-[(18)F]FET) and 4-borono-2-[(18)F]fluoro-l-phenylalanine-fructose (l-[(18)F]FBPA-Fr), to that of [(18)F]FDG in an animal brain tumor model. METHODS: A self-modified automated PET tracer synthesizer was used to produce no-carrier-added (nca) l-[(18)F]FET. The cellular uptake, biodistribution, autoradiography and microPET imaging of l-[(18)F]FET, l-[(18)F]FBPA-Fr and [(18)F]FDG were performed with F98 glioma cell culture and F98 glioma-bearing Fischer344 rats. RESULTS: The radiochemical purity of l-[(18)F]FET was >98% and the radiochemical yield was 50% in average of 16 runs. The uptake of l-[(18)F]FET and l-[(18)F]FBPA-Fr in the F98 glioma cells increased rapidly for the first 5 min and reached a steady-state level after 10 min of incubation, whereas the cellular uptake of [(18)F]FDG kept increasing during the study period. The biodistribution of l-[(18)F]FET, l-[(18)F]FBPA-Fr and [(18)F]FDG in the brain tumors was 1.26+/-0.22, 0.86+/-0.08 and 2.77+/-0.44 %ID/g at 60 min postinjection, respectively, while the tumor-to-normal brain ratios of l-[(18)F]FET (3.15) and l-[(18)F]FBPA-Fr (3.44) were higher than that of [(18)F]FDG (1.44). Both microPET images and autoradiograms of l-[(18)F]FET and l-[(18)F]FBPA-Fr exhibited remarkable uptake with high contrast in the brain tumor, whereas [(18)F]FDG showed high uptake in the normal brain and gave blurred brain tumor images. CONCLUSION: Both l-[(18)F]FET and l-[(18)F]FBPA-Fr are superior to [(18)F]FDG for the brain tumor imaging as shown in this study with microPET.     

Initial characterization of an 18F-labeled myocardial perfusion tracer.

PET allows for quantitative, regional myocardial perfusion imaging. The short half-lives of the perfusion tracers currently in use limit their clinical applicability. Here, the biodistribution and imaging quality of a new 18F-labeled myocardial perfusion agent (18F-BMS-747158-02) in an animal model are described. METHODS: The biodistribution of 18F-BMS-747158-02 was determined at 10 and 60 min after injection. The first-pass extraction fraction of the tracer was measured in isolated rat hearts perfused with the Langendorff method. Small-animal PET imaging was used to study tracer retention. RESULTS: The biodistribution at 10 min after injection demonstrated high myocardial uptake (3.1 percentage injected dose per gram [%ID/g]) accompanied by little activity in the lungs (0.3 %ID/g) and liver (1.0 %ID/g). The tracer showed a high and flow-independent myocardial first-pass extraction fraction, averaging 0.94 (SD = 0.04). PET imaging provided excellent delineation of myocardial structures. The heart-to-lung activity ratio increased from 4.7 to 10.2 between 1 and 15 min after tracer injection (at rest). Adenosine infusion (140 microg/kg/min) led to a significant increase in myocardial tracer retention (from 1.68 [SD = 0.23]) s(-1) to 3.21 [SD = 0.92] s(-1); P = 0.03). CONCLUSION: The observation of a high and flow-independent first-pass extraction fraction promises linearity between tracer uptake and myocardial blood flow. Sustained myocardial tracer uptake, combined with high image contrast, will allow for imaging protocols with tracer injection at peak exercise followed by delayed imaging. Thus, 18F-BMS-747158-02 is a promising new tracer for the quantitative imaging of myocardial perfusion and can be distributed to imaging laboratories without a cyclotron.     

Synthesis and evaluation of O-(3-[18F]fluoropropyl)-L-tyrosine as an oncologic PET tracer

O-(3-[(18)F]fluoropropyl)-L-tyrosine (FPT), an analogue of O-(2-[(18)F]fluoroethyl)-L-tyrosine (FET) as an amino acid tracer for tumor imaging with positron emission tomography (PET), was synthesized and evaluated. FPT was prepared by [(18)F]fluoropropylation of L-tyrosine in a two-step procedure. Biodistribution of FPT was determined in normal mice. FPT, FET and [(18)F]fluorine-2-deoxy-D-glucose (FDG) uptake studies were performed in mice bearing S18 fibrosarcoma and S. aureus-inoculated mice. Also, carcinoma-bearing mice and S. aureus-inoculated mice were imaged using FPT PET imaging compared with FET and FDG PET imaging. Synthesis of FPT was accomplished in about 60 min with an overall radiochemical yield of 25-30% (without decay correction) by manual operation. High uptake and long retention time of FPT and FET in kidney, liver, lung, blood, etc., and low uptake in brain were found. Furthermore, high FPT, FET and FDG uptake in tumor, and almost no FPT and FET uptake in inflammatory tissue, in contrast, high FDG uptake in inflammatory tissue, were observed. In conclusion, FPT is easy to prepare and superior to FDG in the differentiation of tumor and inflammation, and seems to be a potential amino acid tracer like FET for tumors imaging with PET.     

Synthesis and evaluation of l-5-(2-[18F]fluoroethoxy)tryptophan as a new PET tracer

A convenient remote controlled synthesis of a new tryptophan analog, l-5-(2-[¹⁸F] fluoroethoxy)-tryptophan (5-¹⁸FEHTP) was described. The radiochemical yield within 65 min was about 12–16% without decay correction, the radiochemical purity was over 98%, and 5-¹⁸FEHTP dissolved in saline was stable over 6 h at room temperature. The biodistribution of 5-¹⁸FEHTP in mice and the high uptake of 5-¹⁸FEHTP in tumor demonstrated that it is very likely a new PET tracer for tumor imaging.     

Radiosynthesis and biological evaluation of 5-(3-[18F]Fluoropropyloxy)-L-tryptophan for tumor PET imaging

Introduction[¹⁸F]FDG PET has difficulty distinguishing tumor from inflammation in the clinic because of the same high uptake in nonmalignant and inflammatory tissue. In contrast, amino acid tracers do not accumulate in inflamed tissues and thus provide an excellent opportunity for their use in clinical cancer imaging. In this study, we developed a new amino acid tracer 5-(3-[¹⁸F]Fluoropropyloxy)-L-tryptophan ([¹⁸F]-L-FPTP) by two-step reactions and performed its biologic evaluation.Methods[¹⁸F]-L-FPTP was prepared by [¹⁸F]fluoropropylation of 5-hydroxy-L-tryptophan disodium salt and purification on C18 cartridges. The biodistribution of [¹⁸F]-L-FPTP was determined in normal mice and the incorporation of [¹⁸F]-L-FPTP into tissue proteins was investigated. In vitro competitive inhibition experiments were performed with Hepa1-6 hepatoma cell lines. [¹⁸F]-L-FPTP PET imaging was performed on tumor-bearing and inflammation mice and compared with [¹⁸F]-L-FEHTP PET.ResultsThe overall uncorrected radiochemical yield of [¹⁸F]-L-FPTP was 21.1 ± 4.4% with a synthesis time of 60 min, the radiochemical purity was more than 99%. Biodistribution studies demonstrate high uptake of [¹⁸F]-L-FPTP in liver, kidney, pancreas, and blood at the early phase, and fast clearance in most tissues over the whole observed time. The uptake studies in Hepa1-6 cells suggest that [¹⁸F]-L-FPTP is transported by the amino acid transport system B^0,+, LAT2 and ASC. [¹⁸F]-L-FPTP displays good stability and is not incorporated into proteins in vitro. PET imaging shows that [¹⁸F]-L-FPTP can be a better potential PET tracer for differentiating tumor from inflammation than [¹⁸F]FDG and 5-(3-[¹⁸F]fluoroethyloxy)-L-tryptophan ([¹⁸F]-L-FEHTP), with high [¹⁸F]-L-FPTP uptake ratio (2.53) of tumor to inflammation at 60 min postinjection.ConclusionsUsing [¹⁸F]fluoropropyl derivatives as intermediates, the new tracer [¹⁸F]-L-FPTP was achieved with good yield and radiochemical purity, and the biological evaluation results of [¹⁸F]-L-FPTP showed that it was a hopeful tracer for PET tumor imaging.     

18F-fluoroacetate: a potential acetate analog for prostate tumor imaging--in vivo evaluation of 18F-fluoroacetate versus 11C-acetate.

PET with (11)C-acetate ((11)C-ACE) has a high sensitivity for detection of prostate cancer and several other cancers that are poorly detected with (18)F-FDG. However, the short half-life (20.4 min) of (11)C limits the general availability of (11)C-ACE. (18)F-Fluoroacetate ((18)F-FAC) is an analog of acetate with a longer radioactive half-life ((18)F = 110 min). This study was undertaken to assess the potential usefulness of (18)F-FAC as a prostate tumor imaging agent. METHODS: We developed an efficient radiosynthesis for (18)F-FAC, which has already been adapted to a commercial synthesizer. Biodistribution studies of (18)F-FAC were compared with (11)C-ACE in normal Sprague-Dawley male rats and CWR22 tumor-bearing nu/nu mice. We also performed a small-animal PET study of (18)F-FAC in CWR22 tumor-bearing nu/nu mice and a whole-body PET study in a baboon to examine defluorination. RESULTS: We obtained (18)F-FAC in a radiochemical yield of 55% +/- 5% (mean +/- SD) in approximately 35 min and with a radiochemical purity of >99%. Rat biodistribution showed extensive defluorination, which was not observed in the baboon PET, as indicated by the standardized uptake values (SUVs) (SUVs of iliac bones and femurs were 0.26 and 0.3 at 1 h and 0.22 and 0.4 at 2 h, respectively). CWR22 tumor-bearing nu/nu mice showed tumor uptake (mean +/- SD) of 0.78 +/- 0.06 %ID/g (injected dose per gram of tissue) for (11)C-ACE versus 4.01 +/- 0.32 %ID/g for (18)F-FAC. For most organs-except blood, muscle, and fat-the tumor-to-organ ratios at 30 min after injection were higher with (18)F-FAC, whereas the tumor-to-heart and tumor-to-prostate ratios were similar. CONCLUSION: All of these data indicate that (18)F-FAC may be a useful alternative to (11)C-ACE tracer for the detection of prostate tumors by PET.     

Al18F-NOTA-FAPI-04的自动化合成与体内显像

目的:自动化合成Al¹⁸F-1,4,7-三氮杂环壬烷-1,4,7-三乙酸(NOTA)-成纤维细胞激活蛋白抑制剂(FAPI)-04,并进行体内显像,评估其诊断肿瘤的效能。方法:利用All-in-one型自动合成模块合成Al¹⁸F-NOTA-FAPI-04,并进行质量分析;取3只正常BALB/c小鼠和3只4T1小鼠乳腺癌荷瘤小鼠进行PET/CT显像,观察体内Al¹⁸F-NOTA-FAPI-04分布情况;对1例肝细胞肝癌患者(男,51岁)进行Al¹⁸F-NOTA-FAPI-04和18F-FDG PET/CT显像,评估其对肝癌的诊断效能。结果:自动化合成Al¹⁸F-NOTA-FAPI-04的时间约为35 min,合成产率约为(25.2±1.9)%(衰减校正后,n=3),产品为无色透明溶液,pH值为7.0~7.5,其比活度为(46.11±3.07)GBq/μmol(衰减校正后,n=3),放化纯大于99.0%,室温放置6 h后放化纯仍大于98.0%。小鼠体内显像示Al¹⁸F-NOTA-FAPI-04的生理性摄取主要在胆道系统和膀胱中,且高度浓聚于肿瘤病灶区域;肝细胞肝癌患者PET/CT显像示Al¹⁸F-NOTA-FAPI-04和18F-FDG PET/CT在胸骨旁淋巴结、膈上前组淋巴结、肝门区淋巴结、胰十二指肠韧带区淋巴结、腹主动脉旁淋巴结的靶本比值(TBR)分别为4.1、8.9、5.4、4.8、2.2和1.0、2.8、5.0、2.1、1.1。结论:基于All-in-one型自动合成模块合成Al¹⁸F-NOTA-FAPI-04,合成时间较短、产率高、稳定性好,高度浓聚于病灶区域,其PET图像对比度高,诊断性能优异。     

18 F-胆碱类似物的制备及动物体内分布研究

目的 研究肿瘤显像剂^18F标记胆碱类似物2－^18F－氟乙基－二甲基－2－氧乙基铵盐（FECH）。方法 通过两步反应制备FECH。^18F^-与乙二醇二对甲苯磺酸酯发生亲核取代反应，生成2－^18F－氟代乙醇－2－对甲苯磺酸酯，后者与N，N－二甲基乙醇胺反应制成FECH。测定FECH放化纯度及其正常小鼠与荷瘤裸鼠体内生物分布。结果 FECH放射化学产率为25％，总放化合成时间为80min，放射化学纯度＞99％。FECH在小鼠体内血液清除快，肝、肾、膀胱和胰腺有高放射性摄取，脑、心肌、胃、肠道及骨骼放射性摄取较低。有较高的肿瘤／血液、肿瘤／脑、肿瘤／心脏、肿瘤／胃及肿瘤／肌肉放射性比值。结论 ^18F－FECH可望用于某些肿瘤的PET显像。