10011-97-9Relevant academic research and scientific papers
Development of a resonant-type microwave reactor and its application to the synthesis of positron emission tomography radiopharmaceuticals
Kimura, Hiroyuki,Yagi, Yusuke,Ohneda, Noriyuki,Odajima, Hiro,Ono, Masahiro,Saji, Hideo
, p. 680 - 686 (2014)
Microwave technology has been successfully applied to enhance the effectiveness of radiolabeling reactions. The use of a microwave as a source of heat energy can allow chemical reactions to proceed over much shorter reaction times and in higher yields tha
Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK
Davis, Ryan A.,Lau, Kevin,Hausner, Sven H.,Sutcliffe, Julie L.
, p. 8659 - 8663 (2016)
Solid-phase peptide synthesis, head-to-tail cyclization, and subsequent radiolabeling provided a reproducible, simple, rapid synthetic method to generate the cyclic peptide radiotracer cRGDyK([18F]FBA). Herein is reported the first on-resin cyclization and 18F-radiolabeling of a cyclic peptide (cRGDyK) in an overall peptide synthesis yield of 88% (cRGDyK(NH2)) and subsequent radiolabeling yield of 14 ± 2% (decay corrected, n = 4). This approach is generally applicable to the development of an automated process for the synthesis of cyclic radiolabeled peptides for positron emission tomography (PET).
A simplified protocol for the automated production of succinimidyl 4-[ 18F]fluorobenzoate on an IBA Synthera module
Ackermann, Uwe,Yeoh, Shinn Dee,Sachinidis, John I.,Poniger, Stan S.,Scott, Andrew M.,Tochon-Danguy, Henri J.
, p. 671 - 673 (2011)
The important peptide labelling reagent succinimidyl 4-[ 18F]fluorobenzoate ([18F]SFB) has been synthesised in 75-85% decay corrected radiochemical yield using the IBA Synthera platform (IBA Cyclotron Solutions, Louvain-la-neuve, Bel
Synthesis of 18F labelled FK960, a candidate anti-dementia drug, and PET studies in conscious monkeys
Murakami, Yoshihiro,Nishimura, Shintaro,Noda, Akihiro,Harada, Norihiro,Tsukada, Hideo
, p. 1219 - 1228 (2002)
The present study demonstrated the synthesis and in vivo study of 18F-labeled N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide (FK960) which is a novel anti-dementia drug candidate. [18F]FK960 was prepared by a one-pot, three reaction sequence, using nucleophilic fluorination, with an automated synthetic apparatus using either ethyl-4-trimethylammonium triflate (1a) or ethyl-4-nitrobenzoate (lb) as the precursor for labeling. Though la gave a higher yield, the specific activity was 50-100 fold higher with 1b. The radiochemical yield of [18F]FK960 was 7-15% (EOB) and the specific activity ranged from 2.0-60.2GBq/μmol depending on the amount of F-18 used. The synthesis time was 2.2-2.9 h. The obtained [18F]FK960 was injected into 3 conscious monkeys (100-120MBq/kg body weight), and distribution images and pharmacokinetic data for [18F]FK960 showed similar uptake in different brain regions and 3-fold higher levels of [18F]FK960 in blood relative to brain. Copyright
Preparation and evaluation of fluorine-18-labeled insulin as a molecular imaging probe for studying insulin receptor expression in tumors
Kim, Dong Hyun,Blacker, Megan,Valliant, John F.
, p. 3678 - 3686 (2014)
A convenient emulsion-based labeling method was used to synthesize fluorine-18-labeled insulin specifically B1-(4-[18F] fluorobenzoyl)insulin (18F-4b) in 6% overall radiochemical yield in 240 min. In vitro screening in MCF
In vivo positron emission tomography (PET) imaging with an αvβ6 specific peptide radiolabeled using 18F-"click" chemistry: Evaluation and comparison with the corresponding 4-[18F]fluorobenzoyl- and 2-[18
Hausner, Sven H.,Marik, Jan,Gagnon, M. Karen J.,Sutcliffe, Julie L.
, p. 5901 - 5904 (2008)
Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [ 18F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solut
Synthesis and in vitro evaluation of 18F- and 19F-labeled insulin: A new radiotracer for PET-based molecular imaging studies
Guenther, Katharina J.,Yoganathan, Sabesan,Garofalo, Robert,Kawabata, Thomas,Strack, Thomas,Labiris, Renée,Dolovich, Myrna,Chirakal, Raman,Valliant, John F.
, p. 1466 - 1474 (2006)
A new and regioselective strategy was developed for the preparation of fluorine-18-labeled insulin as a novel positron emission tomography (PET) tracer. [18F]-4-Fluorobenzoic acid (4-18FBA), which was produced in 83 ± 8% yield (n = 1
Preparation of the novel fluorine-18-labeled VIP analog for PET imaging studies using two different synthesis methods
Cheng, Dengfeng,Yin, Duanzhi,Zhang, Lan,Wang, Mingwei,Li, Gucai,Wang, Yongxian
, p. 196 - 201 (2007)
Vasoactive intestinal peptide (VIP) receptors are expressed on various tumor cells in much higher density than somatostatin receptors, which provides the basis for radiolabeling VIP as tumor diagnostic agent. However, fast proteolytic degradation of VIP i
[18F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent
Zhang, Bo,Fraser, Benjamin H.,Klenner, Mitchell A.,Chen, Zhen,Liang, Steven H.,Massi, Massimiliano,Robinson, Andrea J.,Pascali, Giancarlo
, p. 7613 - 7617 (2019)
Fluorine-18 is the most utilized radioisotope in positron emission tomography (PET), but the wide application of fluorine-18 radiopharmaceuticals is hindered by its challenging labelling conditions. As such, many potentially important radiotracers remain
Synthesis and liposome encapsulation of a novel 18F-conjugate of ω-conotoxin GVIA for the potential imaging of N-type Ca2+ channels in the brain by positron emission tomography
Azarian, Vahe,Gangloff, Anne,Seimbille, Yann,Delaloye, Sibylle,Czernin, Johannes,Phelps, Michael E.,Silverman, Daniel H. S.
, p. 269 - 283 (2006)
ω-Conotoxin GVIA is a potent, irreversible antagonist of N-type voltage gated Ca2+ channels. A radiofluorinated analogue of GVIA could be useful in assessing regional synaptic density of the brain, in vivo, using positron emission tomography. N
