Fluoridation process for the synthesis of 2-[18f] fluoro-2-deoxy-d ..
09/02/2017 · New high-yield synthesis of 18F-labelled 2-deoxy-2-fluoro-D ..
in the production of 2-[18F]fluoro-2-deoxyglucose
PET imaging is achieved by use of radiotracers, withF-fluoro-2-deoxyglucose (F-FDG) beingcommonly used in clinical practice for evaluation of the metabolicstatus of abnormal and normal tissues (). F-FDG is activelytransported into cells by the same transporters that incorporateglucose (), and is thenphosphorylated by hexokinase 2 (HK2) or glucokinase and convertedto FDG 6-phosphate, which is trapped in the cell immediately afterphosphorylation (). Increasedglucose uptake is characteristic of malignant tumors, becausetumors have increased expression levels of glucose transporters andintracellular enzymes, such as HK2, that are involved in glycolysis().
The potential of the methodology is illustrated by the synthesis of the most important and widelyused [18F]-radiotracer 2-[18F]-fluoro-2-deoxyglucose (FDG) with good radiochemical yield (73%,decay corrected) and superior chemical purity.
Figure 2 Synthesis of 18F-FDG by ..
Representative photomicrographs ofimmunohistochemical staining for hexokinase 2 (HK2) and glucosetransporter 1 (Glut1). A higher HK2 expression was observed in high18F-FDG uptake tumors compared with the low uptake tumorof 18F-FDG in the (A) diethylnitrosamine (DEN model) and(B) hepatitis B virus X protein (HBx-Tg model). The levels of Glut1expression did not differ in the high or low18F-fluoro-2-deoxyglucose (18F-FDG) uptaketumor tissues in the DEN- or HBx-Tg model mice. DEN_high and loware the high and low uptake of 18F-FDG in the DEN model,respectively; HBx_high and low are the high and low uptake of18F-FDG in HBx-Tg model, respectively.
The potential of the methodology is illustrated by the synthesis of the most important and widelyused [18F]-radiotracer 2-[18F]-fluoro-2-deoxyglucose (FDG) with good radiochemical yield (73%,decay corrected) and superior chemical purity. Full text not available from this repository.
FDG - 2-deoxy-2[18F]fluoro-D-glucose | AcronymAttic
Southworth R, Parry CR, Parkes HG, MedinaRA and Garlick PB: Tissue-specific differences in 2-fluoro-2-deoxyglucose metabolism beyond FDG-6-P: a 19F NMRspectroscopy study in the rat. NMR Biomed. 16:494–502. 2003. : :
Okazumi S, Isono K, Enomoto K, et al:Evaluation of liver tumours using fluorine-18-fluorodeoxyglucosePET: characterization of tumor and assessment of effect oftreatment. J Nucl Med. 33:333–339. 1992.
fluoro-2-deoxyglucose-PET (FDG ..
2-fluoro-2-deoxyglucose (FDG) ..
Reagents Kit for production of 2-[18 F]-fluoro-2-deoxy-D-glucose with the AllInOne FDG Synthesis, Pharmaceutical Grade
Synthesis of 18F-2-deoxy-2-fluoro-d ..
compare the cisplatin sensitivity and 18F fluoro-2 deoxy 2 glucose (18F-FDG) ..
Figure 2: Synthesis of 18F-FDG by electrophilic ..
lines and to compare the cisplatin sensitivity and 18F fluoro-2 deoxy 2 glucose (18F-FDG) ..
[18F]FDG resemble those of 2-fluoro ..
Monitoring of tumor progression in(A) diethylnitrosamine (DEN-model) and (B) hepatitis B virus Xprotein (HBx-Tg) model by 18F-fluoro-2-deoxyglucose(18F-FDG) PET/CT. Tumors were first detected inDEN-model mice at 6.5 months after DEN treatment and werelongitudinally observed during hepatocarcinogenesis (at 8.5 and 10months). HBx-Tg model mice were serially imaged after birth from 11to 20 months. Dotted line, H, Bl and asterisk indicate tumors,heart, bladder and non-specific uptake lesion, respectively.
[18F]fluoro-2-deoxyglucose-positron emission …
Representative T2-weighted magneticresonance image (MRI) (upper panel) and18F-fluoro-2-deoxyglucose (18F-FDG) PET/CTimages (lower panel) at 19 months after treatment with (A)diethylnitrosamine (DEN) and of a (B) hepatitis B virus X protein(HBx-Tg model) at 11 months after birth. 18F-FDG PET/CTimages were obtained after MRI acquisition with a T2-weightedsequence. (C and D) Correlation of tumor size and SUVmaxin the DEN and HBx-Tg models, respectively. Dotted line, H andasterisk indicate tumors, heart and stomach, respectively.
Fludeoxyglucose (18F) - Wikipedia
Decreased tumour [18F]2-fluoro-2-deoxy--glucose (18FDG) incorporation is related to response however its significance at the cell level in gastro-oesophageal cancer and how it relates to cell death is unknown. Here human gastric adenocarcinoma (AGS) cells were treated with lethal dose 10 and 50 (LD10 and LD50), determined by using the MTT assay, of the three drugs, epirubicin, 5-fluorouracil and cisplatin, commonly used in the treatment of patients with gastro-oesophageal cancer. 18FDG incorporation was determined after 48 and 72h of treatment with each drug and related to drug-induced changes in glucose transport, hexokinase activity, cell cycle distribution and annexin V-PE binding (a measure of apoptosis). Treatment of cells for 48 and 72h with LD50 doses of cisplatin resulted in reductions in 18FDG incorporation of 27 and 25% respectively and of 5-fluorouracil reduced 18FDG incorporation by 34 and 33% respectively: epirubicin treatment reduced incorporation by 30 and 69% respectively. Cells that had been treated for 72h with each drug were incubated in drug-free media for a further 6 days to determine their ability to recover. Comparison of the ability to recover from the chemotherapy agent, with 18FDG incorporation before the recovery period allowed an assessment of the predictive ability of 18FDG incorporation. Cells treated with either 5-fluorouracil or cisplatin demonstrated recovery on removal of the drug. In contrast, cells treated with epirubicin did not recover corresponding with the greatest 72h treatment decrease in 18FDG incorporation. In contrast to adherent cells treated with cisplatin or 5-fluorouracil, adherent epirubicin-treated cells also exhibited very high levels of apoptosis. Glucose transport was decreased after each treatment whilst hexokinase activity was only decreased after 72h of treatment with each drug. There was no consistent relationship observed between 18FDG incorporation and cell cycle distribution. Our results show that at the tumour cell level in gastric tumour cells, decreased 18FDG incorporation and glucose transport, accompanies therapeutic growth inhibition. 18FDG incorporation is particularly diminished in cells exhibiting apoptosis.
Labeled 2‐deoxy‐D‐glucose analogs
A number of studies (; ; ; ) have demonstrated that a reduction in tumour uptake of the glucose analogue, [18F]2-fluoro-2-deoxy--glucose (18FDG), is observed during and upon completion of chemotherapy in gastro-oesophageal cancer. Although decreased tumour 18FDG uptake has been shown to be associated with response (and may in fact predict tumour response), its significance at the gastro-oesophageal tumour cell level is not known. Response to chemotherapy, as seen on 18FDG-PET with a corresponding reduction in uptake in solid tumours, may be related to a decrease in tumour cellularity or a decrease in 18FDG uptake per cell, or a combination of both. In solid tumours, tumour cells can recover and it is not known if this decreased 18FDG uptake during response is due to modulation in 18FDG uptake by cells that will not recover. This reduction in cellular uptake of 18FDG may occur prior to reduction in tumour volume and therefore may reflect apoptosis. To further confuse matters, a flare phenomenon has been recorded in the early period following exposure to chemotherapy (). In addition chemotherapy may alter 18FDG cellular uptake by hexokinase (HK) and/or glucose transport modulation.
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