• Title/Summary/Keyword: $[^{18}F]F_2$

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Synthesis and Evaluation of $2-[^{18}F]Fluoro-A85380$, a Radioligand for ${\alpha}_4{\beta}_2$ Nicotinic Acetylcholine Receptor Imaging (${\alpha}_4{\beta}_2$ 니코틴성 아세틸콜린 수용체 영상 방사성리간드 $2-[^{18}F]fluoro-A85380$의 합성 및 평가)

  • Ryu, Eun-Kyoung;Choe, Yearn-Seong;Kim, Sang-Eun;Hwang, Sae-Hwan;Paik, Jin-Young;Choi, Yong;Lee, Kyung-Han;Kim, Byung-Tae
    • The Korean Journal of Nuclear Medicine
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    • v.36 no.4
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    • pp.261-270
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    • 2002
  • Purpose: Nicotinic acetylcholine receptors (nAChRs), which mediate excitatory neurotransmission, are known to participate in various neurophysiological functions. Severe losses of nAChRs have been noted in Alzheimer's and Parkinson's diseases. Therefore, noninvasive and quantitative imaging of nAChRs would offer a better understanding on the function of these receptors. In this study, $2-[^{18}F]fluoro-A85380\;([^{18}F]1)$, an ${\alpha}_4{\beta}_2$ nAChRs radioligand, was prepared using one HPLC purification and evaluated in mouse brain, and the results were compared with those in the literature. Materials and Methods: $[^{18}F]1$ was prepared by $[^{18}F]$fluorination of the iodo precursor followed by acidic deprotection and then purified by HPLC. Tissue distribution studies were performed in mouse brain at the indicated time points and the result was expressed as %ID/g. Inhibition studies were also carried out with pretreatment of various ligands. Results: One HPLC purification method gave the desired product in 15-20% radiochemical yield and with high specific activity ($38-55GBq/{\mu}mol$). Tissue distribution studies showed that $[^{18}F]1$ specifically labeled nAChRs in mouse brain with a high thalamus to cerebellum uptake ratio (13.8 at 90 min). Inhibition studios demonstrated selective binding of $[^{18}F]1$ to nAChRs, blocking the uptake of the $[^{18}F]1$ in nAChR-rich legions by selective ligands such as cytisine and nicotine which are well-known nAChRs agonists. Conclusion: This study demonstrated that the $[^{18}F]1$ produced by the method using one HPLC purification gave the results similar to those reported in the literature. Therefore, this synthetic method can be readily applied to the routine preparation of $[^{18}F]1$, a PET radioligand for ${\alpha}_4{\beta}_2$ nAChRs imaging.

Differential Diagnosis of Breast Mass and Staging of Breast Cancer Using F-18-FDG PET (F-18-FDG PET을 이용한 유방종괴의 감별진단과 유방암의 병기설정)

  • Yeo, Jeong-Seok;Lee, Dong-Soo;Kang, Keon-Wook;Noh, Dong-Young;Chung, June-Key;Lee, Myung-Chul
    • The Korean Journal of Nuclear Medicine
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    • v.33 no.6
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    • pp.502-511
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    • 1999
  • Purpose: F-18-fluorodeoxyglucose (FDG) positron emission tomography (PET) has been proven to be useful in the differential diagnosis of breast mass and staging of breast cancer. This study assessed the diagnostic accuracy of F-18-FDG PET in the differentiation of breast mass and staging of breast cancer. Materials and Methods: Total 42 patients who had breast mass underwent F-18-FDG PET (all female, 40: 10 year old). We compared F-18 FDG PET results with pathologic findings in 24 patients Results: In the differentiation of breast mass, sensitivity and specificity were 95% (19/20) and 77% (7/9) respectively. Three false positive cases were due to inflammation and one false negative patient had small tumor less than 1 cm. In the assessment of axillary lymph node status, sensitivity and specificity were 73% (8/11) and 100% (7/7) respectively. We found distant metastasis that were not suspected before F-18-FDG PET in 2 patients. Conclusion: F-18-FDG PET shows good diagnostic performance in differentiation of breast mass and staging of breast cancer.

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Synthesis and Biodistribution of Flumazenil Derivative [F-18](3-(2-Fluoro) flumazenil for Imaging Benzodiazepine Receptor (벤조디아제핀 수용체 영상용 양전자 방출 핵종 표지 플루마제닐 유도체 [F-18](3-(2-Fluoro)flumazenil의 합성과 생체 내 분포)

  • Hong, Sung-Hyun;Jeong, Jae-Min;Chang, Young-Soo;Lee, Dong-Soo;Chung, June-Key;Cho, Jung-Hyuck;Lee, Sook-Ja;Kang, Sam-Sik;Lee, Myung-Chul
    • The Korean Journal of Nuclear Medicine
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    • v.33 no.6
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    • pp.527-536
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    • 1999
  • Purpose: Radiotracers that bind to the central benzodiazepine receptor are useful for the investigation of various neurological and psychiatric diseases. [C-11]Flumazenil, a benzodiazepine antagonist, is the most widely used radioligand for central benzodiazepine receptor imaging by PET. We synthesized 3-(2-[F-18]fluoro)flumazenil, a new fluorine-18 ($t_{1/2}$= 110 min) labeled analogue of benzodiazepine receptor imaging agent, and evaluated in vivo for biodistribution in mice. Materials and Methods: Flumazenil (Ro 15-1788) was synthesized by a modification of the reported method. Precursor of 3-(2-[F-18]fluoro)flumazenil, the tosylated flumazenil derivative was prepared by the tosylation of the ethyl ester by ditosylethane. [F-18] labeling of tosyl substitued flumazenil precursor was performed by adding F-18 ion at $85^{\circ}C$ in the hot ceil for 20 min. The reaction mixture was trapped by C18 cartridge, washed with 10% ethanol, and eluted by 40% ethanol. Bidistribution in mice was determined after intravenous injection. Results: The total chemical yield of tosylated flumazenil derivative was ${\sim}40%$. The efficiency of labeling 3-(2-[F-18]fluoro)flumazenil was 66% with a total synthesis time of 50 min. Brain uptakes of 3-(2-[F-18]fluoro)flumazenil at 10, 30, 60 min after injection, were $2.5{\pm}0.37,\;2.2{\pm}0.26,\;2.1{\pm}0.11$ and blood activities were $3.7{\pm}0.43,\;3.3{\pm}0.07,\;3.3{\pm}0.09%ID/g$, respectively. Conclusion: We synthesized a tosylated flumazenil derivative which was successfully labeled with no-carrier-added F-18 by nucleophilic substitution.

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Synthesis and $^{18}F$ Labelling of Organic Ammonium Salts to New Cardiac Flow Tracer for PET and Their Biodistribution (양전자단층촬영에 이용 가능한 새로운 심근 혈류 추적자 개발; F-18이 표지된 유기암모늄염의 합성과 체내분포에 관한 연구)

  • Yu, Kook-Hyun
    • The Korean Journal of Nuclear Medicine
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    • v.28 no.3
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    • pp.331-337
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    • 1994
  • In order to develop a $^{18}F$-labelled myocardial perfusion agent(flow tracer) for PET, $^{18}F$-labelled organic ammonium cations were synthesized and evaluated in relation to their biodistribution. Five quaternary organic ammonium compounds were labelled with $^{18}F$ in a side chain with moderate to good yields by direct introduction of $^{18}F$-fluoride. Radiochemical yields have been achieved in 30-40min by the precursors (tosylates) in dimethylsulfoxide 15-60% (decay corrected). The reaction was found to be autocatalyzed. A remote controlled procedure was developed in these synthesis. $^{18}F$-Labelling and HPLC-purification of com-pounds needed about 60 min(Yield; 7-20%). Up to now the two compounds N-4-[$^{18}F$]fluorobutyl-pyridinium cation(1) and N, N dibenzyl-4(2-[$^{18}F$]fluoroethyl)piperidinium cation(2) were investigated in relation to their biodistribution in mice. Compound 1 showed at 1 min post injection the high uptake of 19.22% ID/g organ in the myocardium but a following fast decline to 1.12% ID/g organ after 40min. Uptake of compound 2 was after 1min in the heart 5.90% ID/g organ but after 40min at the relative high value of 4.33% ID/g organ. Heart:blood ratio for compound(1) at 1 min was 8.3, at 40 min 2.6 for compound II 2.0(1min) and 15.0(40 min). As data of compound 2 showed greater heart uptake, slower myocardial release, and higher heart: blood ratios, compound 2 is a good candidate for further evaluation.

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Synthesis of a Dopamine Transporter Imaging Agent, N-(3-[$^{18}F$]fluoropropyl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-iodophenyl)nortropane (도파민운반체 방사성추적자 N-(3-[$^{18}F$Fluoropropyl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-iodophenyl)nortropane의 합성)

  • Choe, Yearn-Seong;Oh, Seung-Jun;Chi, Dae-Yoon;Kim, Sang-Eun;Choi, Yong;Lee, Kyung-Han;Kim, Byung-Tae
    • The Korean Journal of Nuclear Medicine
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    • v.33 no.3
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    • pp.298-305
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    • 1999
  • Purpose: N-(3-[$^{18}F$]Fluoropropyl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-iodophenyl)nortropane [$^{18}F$]FP-CIT) has been shown to be very useful for imaging the dopamine transporter. However, synthesis of this radiotracer is somewhat troublesome. In this study, we used a new method for the preparation of [$^{18}F$]FP-CIT to increase radiochemical yield and effective specific activity. Materials and Methods: [$^{18}F$]FP-CIT was prepared by N-alkylation of nor-${\beta}$-CIT (2 mg) with 3-bromo-1-[$^{18}F$]fluoropropane in the presence of $Et_3N$ (5-6 drops of $DMF/CH_3CN$, $140^{\circ}C$, 20 min). 3-Bromo-1-[$^{18}F$]fluoropropane was synthesized from $5{\mu}L$ of 3-bromo-1-trifluoromethanesulfonyloxypropane (3-bromopropyl-1-triflate) and $nBu_4N^{18}F$ at $80^{\circ}C$. The final compound was purified by reverse phase HPLC and formulated in 13% ethanol in saline. Results: 3-Bromo-1-[$^{18}F$]fluoropropane was obtained from 3-bromopropyl-1-triflate and $nBu_4N^{18}F$ in 77-80% yield. N-Alkylation of nor-${\beta}$-CIT with 3-bromo-1-[$^{18}F$]fluoropropane was carried out at $140^{\circ}C$ using acetonitrile containing a small volume of DMF as the solvents. The overall yield of [$^{18}F$]FP-CIT was 5-10% (decay-corrected) with a radiochemical purity higher than 99% and effective specific activity higher than the one reported in the literature based on their HPLC data. The final [$^{18}F$]FP-CIT solution had the optimal pH (7.0) and it was pyrogen-free. Conclusion: In this study, 3-bromopropyl-1-triflate was used as the precursor for the [$^{18}F$]fluorination reaction and new conditions were developed for purification of [$^{18}F$]FP-CIT by HPLC. We established this new method for the preparation of [$^{18}F$]FP-CIT, which gave high effective specific activity and relatively good yield.

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A Study on Minimizing the Residual $^{18}F$-FDG in the Tubing Using Nitrogen Gas (FDG 합성 후 질소가스를 이용한 튜빙의 잔류 $^{18}F$-FDG 최소화를 위한 방법의 유용성)

  • Kim, Dong-Il;Park, Hoon;Seok, Jae-Dong
    • The Korean Journal of Nuclear Medicine Technology
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    • v.14 no.1
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    • pp.8-12
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    • 2010
  • Purpose: In $^{18}F$-FDG automated synthesizer, deliver is done in automated mode after synthesis until the dispenser. After the delivery, the yield is calculated from the radioactivity which was read by the dose calibrator located in the dispenser. However, when the distance between the automated synthesizer and the dispenser is far, there are $^{18}F$-FDG residues, which results in loss of the amount of $^{18}F$-FDG. This study investigated the usefulness of a method that minimizes $^{18}F$-FDG residues. Materials and Methods: The structure of the tubing between the (TRACERlab Mx FDG; GE.) and the dispenser is that the distance is 8 m and the internal diameter is 1/16 inch. The synthesis process of The module goes through the synthesis process of trap, synthesis, delivery in the automated module. The time taken for synthesis is about 25 to 26 minutes, after which rinsing is done. However, after rinsing, as the distance of the tubing increased, there were 10~13% of $^{18}F$-FDG residues. Therefore, a method of using push syringe and $N_2$ gas in manual mode to minimize $^{18}F$-FDG residues is analyzed. Results: In manual mode, there were $^{18}F$-FDG residues of 4~5% for the push syringe, and there were $^{18}F$-FDG residues of less than 1% for the $N_2$ gas, which showed that the method using $N_2$ gas had superior usefulness. Also, there were no $^{18}F$-FDG residues in the cleaning the next day. Conclusion: The distance between the synthesizer and the dispenser needs to be reduced as much as possible, to reduce the rate of loss of $^{18}F$-FDG resulting from the distance of the tubing. However, in case the distance between the synthesizer and the dispenser has to be increased due to the system structure, using push syringe and $N_2$ gas simultaneously is a useful method for minimizing $^{18}F$-FDG residues.

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Synthesis of [18F]Fluorocholine Analogues as a Potential Imaging Agent for PET Studies

  • Yu, Kook-Hyun;Park, Jeong-Hoon;Yang, Seung-Dae
    • Bulletin of the Korean Chemical Society
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    • v.25 no.4
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    • pp.506-510
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    • 2004
  • There have been intensive studies concerning $[^{11}F]$choline ($[^{11}F]$methyldimethyl( ${\beta}$ -hydroxyethyl) ammonium) (1) which is known as a very effective tracer in imaging various human tumors localized in brain, lung, esophagus, rectum, prostate and urinary bladder using Positron Emission Tomography (PET) and there is increasing interest in $^{18}F$ labelled choline (2) and proved to be useful to visualize prostate cancer. We have prepared six $^{18}F$ labelled alkyl choline derivatives (3a-3c, 4a-4c) from ditosylated and dibrominated alkanes in moderate yields. The six alkyl tosylate or bromate ammonium salts have been synthesized as precursors. Radiofluorination was achieved by the treatment of precursors with $^{18}F$ - in the presence of Kryptofix-2.2.2.. The labeling yields varied ranging from 7 to 25%.

Performance of the RI Exhaust Filter at Chosun University Cyclotron Facility and 18F Emission Reduction (조선대학교 사이클로트론 시설의 RI 배기필터 성능평가 및 18F 배출저감 연구)

  • Jeong, Cheol-Ki;Jang, Han;Lee, Goung-Jin
    • Journal of Radiation Industry
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    • v.11 no.1
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    • pp.13-18
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    • 2017
  • Recently, the number of PET cyclotrons has increased in Korea. A cyclotron mainly produces $^{18}F$, which is used for the production of [$^{18}F$]FDG, a cancer diagnostic radiopharmaceutical. For radiation protection, the discharge control standard under the Nuclear Safety Act limits the radioactive concentration of $^{18}F$ in the exhaust discharged from a nuclear power utilization facility to below $2,000Bq\;m^{-3}$. However, the radioactive concentration of $^{18}F$ discharged during [$^{18}F$]FDG production at the cyclotron facility at Chosun University is maintained at about $1,500Bq\;m^{-3}$ on average, which is 75% of the concentration limit of the discharge control standard, and temporarily exceeds the standard as per the real-time monitoring results. This study evaluated the performance of the exhaust filter unit of the cyclotron facility at Chosun University by assessing the concentration of $^{18}F$ in the exhaust, and an experiment was conducted on the discharge reduction, where $^{18}F$ is discharged without reacting with the FDG precursors during [$^{18}F$]FDG synthesis and is immediately captured by the [$^{18}F$]FDG automatic synthesis unit. Based on the performance evaluation results of the exhaust filter at the cyclotron facility of Chosun University, the measured capture efficiency before and after the filter was found to be 92%. Furthermore, the results of the discharge reduction experiment, where the exhaust $^{18}F$ was immediately captured by the [$^{18}F$]FDG synthesizer, showed a very satisfactory 94.3% reduction in the concentration of discharge compared to the existing discharge concentration.

A Study of Convergence Social Voluntary Service Activity and Sense of Profession Values, Self-Esteem, Sociality in Nursing Students (간호대학생의 융·복합 사회봉사활동과 직업가치관, 자아존중감, 사회성에 관한 연구)

  • Yoon, Mi-Sun;Yim, So-youn
    • The Journal of the Korea Contents Association
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    • v.18 no.11
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    • pp.562-570
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    • 2018
  • This study is a descriptive research to understand the degree and relevance of profession value, self - esteem, and sociality of nursing college students according to voluntary service activities. The results showed that the formation of profession values according to the general characteristics was related to religion (F = 4.79, p = .003) and major (F = 3.75, p = .011) and self esteem was related to grade (F = 4.84, p = .002). The profession values according to the characteristics of voluntary service activities showed a significant difference in volunteer time (F=18.70, p<.001), volunteer duration (F=18.87, p<.001), volunteer organization(F=3.41, p=.001), volunteer motivation(F=8.08, p<.001), participation path(F=3.63, p=.002), participation field(F = 2.13, p = .031). The profession value was positively correlated with self-esteem(r = .327, p <.01) and sociality(r= .248, p <.01). Self-esteem showed a statistically significant positive correlation with sociality(r= .327, p <.01).

Quality Control of Residual Solvents in $[^{18}F]$FDG Preparations by Gas Chromatography (기체 크로마토그래피를 이용한 $[^{18}F]$FDG 주사액 중의 잔류 용매의 정도관리)

  • Lee, Hak-Jeong;Jeong, Jae-Min;Lee, Yun-Sang;Kim, Hyung-Woo;Chang, Young-Soo;Lee, Dong-Soo;Chung, June-Key;Lee, Myung-Chul
    • Nuclear Medicine and Molecular Imaging
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    • v.41 no.6
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    • pp.566-569
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    • 2007
  • Purpose: Analysis of volatile organic solvents in 2-deoxy-2-$[^{18}F]$ fluoro-D-glucose ($[^{18}F]$FDG) preparations was performed by gas chromatography (GC), in accordance with USP. Materials and Methods: Analyses were carried out on a Hewlett-Packard 6890 gas chromatography equipped with an FID. Results: We determined the amounts of ethanol and acetonitrile on every batch of our routine $[^{18}F]$FDG preparations, ranging between 5000 ppm and 100 ppm. In our routine preparation of $[^{18}F]$FDG, the amount of acetonitrile and ethanol in the final product were well below the maximum allowable limit described in the USP. Conclusion: Our $[^{18}F]$FDG preparations were in accordance with the suggested USP maximum allowable levels of the quality control analysis of volatile organic compounds.