• Title/Summary/Keyword: radiopharmaceuticals

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The targeting peptides for tumor receptor imaging

  • Yim, Min Su;Ryu, Eun Kyoung
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.2 no.2
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    • pp.63-68
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    • 2016
  • Peptides have been developed for in vivo imaging probes against to the specific biomarker in the biological process of living systems. Peptide based imaging probes have been applied to identify and detect their active sites using imaging modalities, such as PET, SPECT and MRI. Especially, tumor receptor imaging with the peptides has been widely used to specific tumor detection. This review discusses the targeting peptides that have been successfully characterized for tumor diagnosis by receptor imaging.

A pyrazolopyrimidine-based radioligand for imaging of the translocator protein

  • Kwon, Young-Do;Kim, Hee-Kwon
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.2 no.2
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    • pp.69-72
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    • 2016
  • Since the translocator protein (TSPO) is involved in neurodegeneration diseases, many scientists' interest has been focused on the development of a ligand targeting TSPO. A novel compound based on pyrazolo[1,5 -a] pyrimidine structure, DPA-714, has been studied and considered as a TSPO ligand with high affinity. In this highlight review, several researches for the novel radioligand for the translocator protein are illustrated.

Fully automated ethanolic loop synthesis of the [11C]OMAR

  • Jang, Keun Sam;Song, Ho-Chun
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.2 no.2
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    • pp.137-142
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    • 2016
  • We have successfully synthesized of 4-cyano-1-(2,4-dichlorophenyl)-5-(4-[$^{11}C$]methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxzmide ([$^{11}C$]OMAR), which has been shown a progressing candidate to human brain PET study, from fully automated loop method using ethanol as the only solvent for the entire manufacturing process. The radiochemical yield of [$^{11}C$]OMAR was observed in $4.1{\pm}0.2%$ with $4990{\pm}384Ci/mmol$ of the specific activity and total synthesis time was about 45 minutes after HPLC purification (n = 3, decay corrected) from ethanolic loop system, which was exhibited to better results compared with conventional methods. Ethanolic loop chemistry is favorable and efficient method by simplifies manufacturing procedures as well as satisfied suitable for human administration.

Development of fluorination methodology for carbon-fluorine bond formation: old electrophilic fluorinating reagents

  • Bae, Dae Young;Lee, Eunsung
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.4 no.1
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    • pp.11-15
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    • 2018
  • Electrophilic fluorinating reagents are typically efficient for carbon-fluorine (C-F) bonds formation due to their higher reactivity even under mild condition. Thus, they have been playing an important role to improve C-F bonds formation reactions via direct fluorination reaction with electrophilic fluorinating reagents or transition metal catalysis. Advances on the recent fluorination methods are mainly results of $Selectfluor^{TM}$'s capability on facile fluorination. In this mini-review, we describe synthesis and application of four old yet popular electrophilic fluorinating reagents such as N-fluorobenzenesulfonimide (NFSI), N-fluoropyridinium salts, $Selectfluor^{TM}$, and N-fluorosultam.

Molecular imaging of atherosclerosis using reporter gene system

  • Yoo, Ran Ji;Lee, Kyochul;Kang, Joo Hyun;Lee, Yong Jin
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.4 no.1
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    • pp.26-31
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    • 2018
  • Macrophages play a key role in atherosclerotic plaque formation, but their participation has been discerned largely via ex vivo analyses of atherosclerotic lesions. Therefore, we aimed to identify atherosclerosis on noninvasive in vivo imaging using reporter gene system. This study demonstrated that recruitment of macrophages could be detected in atherosclerotic plaques of Apolipoprotein E knockout (ApoE-/-) mice with a sodium iodide symporter (NIS) gene imaging system using $^{99m}Tc-SPECT$. This novel approach to tracking macrophages to atherosclerotic plaques in vivo could have applications in studies of arteriosclerotic vascular disease.

Radiolabeled single-domain antibody for tumor receptor imaging

  • Moon, Yeajin;Lee, Ju Young;Ryoo, Woonseok;Seo, Seung-Yong
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.6 no.1
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    • pp.39-45
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    • 2020
  • Recently, single-domain antibodies (sdAb) are bioengineered for molecular imaging applications. Single-domain antibody, obtained from naturally occurring antibodies in camelid species and cartilaginous fish is the smallest fully functional antigen-binding antibody fragments of heavy-chain. Since their discovery, they have been investigated extensively in clinical therapeutics, monitoring and diagnostics. Their small size is important advantage for high solubility, high stability, fast blood clearance and rapid targeting. This review article summarizes the recent status of this new antibody to visualize, diagnose or inhibit specific targets of cancer.

Suggestion for Good Manufacturing Practice of Radiopharmaceuticals (우수방사성의약품 제조관리를 위한 제언)

  • Shin, Byungchul;Lee, Sangbock
    • Journal of the Korean Society of Radiology
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    • v.7 no.6
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    • pp.397-402
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    • 2013
  • This study suggests considerations for legislation of radiopharmaceutical manufacturing practice according as the Korea Pharmaceutical Affairs Act and guidelines on foreign radiopharmaceutical manufacturing practice. Pharmaceuticals should be verified safety, effectiveness, and uniformity. Therefore, it is expected that the efficiency of the administration of radiopharmaceuticals increase and nation's health promote if rational manufacturing management to consider of radiopharmaceutical properties is legislated.

Strain-promoted alkyne-azide cycloaddition for PET molecular imaging study

  • Jeong, Hyeon Jin;Kim, Dong Wook
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.1 no.1
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    • pp.15-22
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    • 2015
  • $^{18}F$-labeling reaction of bioactive molecule via click chemistry is widely used to produce $^{18}F$-labeled radiotracer in the field of radiopharmaceutical science and molecular imaging. In particular, bioorthogonal strain-promoted alkyne-azide cycloaddition (SPAAC) reaction has received much attention as an alternative ligation method for radiolabeling bioactive molecules such as peptides, DNA, proteins as well as nanoparticles. Moreover, SPAAC based pretargeting method could provide tumor images successfully on positron emission tomography system using nanoparticle such as mesoporous silica nanoparticles.

Synthesis of 68Ga-labeled gold nanoparticles for tumor targeted positron emission tomography imaging

  • Jeon, Jongho;Choi, Mi Hee
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.1 no.1
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    • pp.46-52
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    • 2015
  • Herein we present the synthesis of $^{68}Ga$-labeled gold nanoparticles for in vivo PET imaging. A novel chelator DTPA-Cys was easily prepared from diethylenetriaminepentaacetic dianhydride in high yield. The ${\alpha}_v{\beta}_3$ integrin receptor targeted gold nanoparticle probe was synthesized by using DTPA-Cys, polyethylene glycol and cRGD peptide. $^{68}Ga$ labeling of cRGD conjugated gold nanoparticle was carried out at $40^{\circ}C$ for 30 min. Observed radiochemical yield was more than 75% as determined by radio-TLC and the probe was purified by centrifugation. In vitro stability test showed that 90% of $^{68}Ga$-labeled gold nanoparticle probe was stable in FBS for 1 h. Those results demonstrated that $^{68}Ga$-labeled gold nanoparticle could be used as a potentially useful probe for specific tumor imaging.

Imaging Hypoxic Myocardium (심근 저산소증 영상)

  • Bae, Sang-Kyun
    • The Korean Journal of Nuclear Medicine
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    • v.39 no.2
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    • pp.141-145
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    • 2005
  • Hypoxia (decreased tissue oxygen tension) is a component of many diseases such as tumors, cerebrovascular diseases and ischemic heart diseases. Although hypoxia can be secondary to a low inspired $pO_2$ or a variety of lung disorders, the most common cause is ischemia due to an oxygen demand greater than the local oxygen supply. In the heart tissue, hypoxia is often observed in persistent low-flow states, such as hibernating myocardium. Direct "hot spot" imaging of myocardial tissue hypoxia is potentially of great clinical importance because it may provide a means of identifying dysfunctional chronically ischemic but viable hibernating myocardium. A series of radiopharmaceuticals that incorporate nitroimidazole moieties have been synthesized to detect decreased local tissue pO2. In contrast to agents that localize in proportion to perfusion, these agents concentrate in hypoxic tissue. However, the ideal agents are not developed yet and the progress is very slow. Furthermore, the research focus is on tumor hypoxia nowadays. This review introduces the myocardial hypoxia imaging with summarizing the development of radiopharmaceuticals.