scholarly journals [18F]Fluoroalkyl azides for rapid radiolabeling and (Re)investigation of their potential towards in vivo click chemistry

2017 ◽  
Vol 15 (28) ◽  
pp. 5976-5982 ◽  
Author(s):  
Christoph Denk ◽  
Martin Wilkovitsch ◽  
Philipp Skrinjar ◽  
Dennis Svatunek ◽  
Severin Mairinger ◽  
...  
Keyword(s):  

[18F]Fluoroalkyl azides were developed as efficient click agents for rapid radiolabeling, and (re)investigated towards application in pretargeted PET imaging.

2016 ◽  
Vol 27 (7) ◽  
pp. 1707-1712 ◽  
Author(s):  
Christoph Denk ◽  
Dennis Svatunek ◽  
Severin Mairinger ◽  
Johann Stanek ◽  
Thomas Filip ◽  
...  

ChemBioChem ◽  
2020 ◽  
Vol 21 (19) ◽  
pp. 2836-2843 ◽  
Author(s):  
Neil Gerard Quigley ◽  
Stefano Tomassi ◽  
Francesco Saverio Leva ◽  
Salvatore Di Maro ◽  
Frauke Richter ◽  
...  

Author(s):  
Qinheng Zheng ◽  
Hongtao Xu ◽  
Hua Wang ◽  
Wen-Ge Han Du ◽  
Nan Wang ◽  
...  

The lack of simple, efficient [<sup>18</sup>F]fluorination processes and new target-specific organofluorine probes remains the major challenge of fluorine-18-based positron emission tomography (PET). We report here a fast isotopic exchange method for the radiosynthesis of aryl [<sup>18</sup>F]fluorosulfate based PET agents enabled by the emerging sulfur fluoride exchange (SuFEx) click chemistry. The method has been applied to the fully-automated <sup>18</sup>F-radiolabeling of twenty-five structurally diverse aryl fluorosulfates with excellent radiochemical yield (83–100%) and high molar activity (up to 281 GBq µmol<sup>–1</sup>) at room temperature in 30 seconds. The purification of radiotracers requires no time-consuming high-performance liquid chromatography (HPLC), but rather a simple cartridge filtration. The utility of aryl [<sup>18</sup>F]fluorosulfate is demonstrated by the <i>in vivo</i> tumor imaging by targeting poly(ADP-ribose) polymerase 1 (PARP1).


2008 ◽  
Vol 1 (2) ◽  
pp. 110-114 ◽  
Author(s):  
A. Gee ◽  
L. Martarello ◽  
J. Passchier ◽  
M. Wishart ◽  
C. Parker ◽  
...  
Keyword(s):  

2021 ◽  
Author(s):  
Cinzia Marceddu ◽  
Adam Hartley ◽  
Mikhail Caga-Anan ◽  
Samata Pandey ◽  
Yasmin Morris ◽  
...  

2019 ◽  
Vol 6 (1) ◽  
Author(s):  
Carlos Velasco ◽  
Adriana Mota-Cobián ◽  
Jesús Mateo ◽  
Samuel España

Abstract Background Multi-tracer positron emission tomography (PET) imaging can be accomplished by applying multi-tracer compartment modeling. Recently, a method has been proposed in which the arterial input functions (AIFs) of the multi-tracer PET scan are explicitly derived. For that purpose, a gamma spectroscopic analysis is performed on blood samples manually withdrawn from the patient when at least one of the co-injected tracers is based on a non-pure positron emitter. Alternatively, these blood samples required for the spectroscopic analysis may be obtained and analyzed on site by an automated detection device, thus minimizing analysis time and radiation exposure of the operating personnel. In this work, a new automated blood sample detector based on silicon photomultipliers (SiPMs) for single- and multi-tracer PET imaging is presented, characterized, and tested in vitro and in vivo. Results The detector presented in this work stores and analyzes on-the-fly single and coincidence detected events. A sensitivity of 22.6 cps/(kBq/mL) and 1.7 cps/(kBq/mL) was obtained for single and coincidence events respectively. An energy resolution of 35% full-width-half-maximum (FWHM) at 511 keV and a minimum detectable activity of 0.30 ± 0.08 kBq/mL in single mode were obtained. The in vivo AIFs obtained with the detector show an excellent Pearson’s correlation (r = 0.996, p < 0.0001) with the ones obtained from well counter analysis of discrete blood samples. Moreover, in vitro experiments demonstrate the capability of the detector to apply the gamma spectroscopic analysis on a mixture of 68Ga and 18F and separate the individual signal emitted from each one. Conclusions Characterization and in vivo evaluation under realistic experimental conditions showed that the detector proposed in this work offers excellent sensibility and stability. The device also showed to successfully separate individual signals emitted from a mixture of radioisotopes. Therefore, the blood sample detector presented in this study allows fully automatic AIFs measurements during single- and multi-tracer PET studies.


Sign in / Sign up

Export Citation Format

Share Document