1454889-24-7Relevant academic research and scientific papers
Synthesis and Characterization of Fluorine-18-Labeled N-(4-Chloro-3-((fluoromethyl- d2)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain
Wang, Junfeng,Qu, Xiying,Shoup, Timothy M.,Yuan, Gengyang,Afshar, Sepideh,Pan, Chuzhi,Zhu, Aijun,Choi, Ji-Kyung,Kang, Hye Jin,Poutiainen, Pekka,El Fakhri, Georges,Zhang, Zhaoda,Brownell, Anna-Liisa
, p. 3381 - 3389 (2020/04/17)
We have synthesized and characterized [18F]-N-(4-chloro-3-((fluoromethyl-d2)thio)phenyl)-picolinamide ([18F]15) as a potential ligand for the positron emission tomography (PET) imaging of mGluR4 in the brain. Radioligand [
MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 4
-
Page/Page column 48-49, (2020/07/25)
The present application provides picolinamide compounds that can be used as allosteric positron emission tomography ("PET") imaging probes. Methods of using these compounds for treating a neurodegenerative disease are also provided.
HPLC-free: In situ 18F-fluoromethylation of bioactive molecules by azidation and MTBD scavenging
Lu, Yingqing,Choi, Ji Young,Kim, Sang Eun,Lee, Byung Chul
, p. 11798 - 11801 (2019/10/02)
Sequential usage of azide and MTBD, which generates pure [18F]fluoromethyl tosylate and scavenges unreacted desmethyl precursors, provided an efficient HPLC-free strategy for the radiosynthesis of 18F-fluoromethylated compounds with
Identification and in vivo evaluation of a fluorine-18 rolipram analogue, [18F]MNI-617, as a radioligand for PDE4 imaging in mammalian brain
Thomae, David,Morley, Thomas J.,Lee, Hsiaoju S.,Barret, Olivier,Constantinescu, Cristian,Papin, Caroline,Baldwin, Ronald M.,Tamagnan, Gilles D.,Alagille, David
, p. 205 - 213 (2016/05/09)
Phosphodiesterase (PDE) 4 is the most prevalent PDE in the central nervous system (CNS) and catalyzes hydrolysis of intracellular cAMP, a secondary messenger. By therapeutic inhibition of PDE4, intracellular cAMP levels can be stabilized, and the symptoms of psychiatric and neurodegenerative disorders including depression, memory loss and Parkinson's disease can be ameliorated. Radiotracers targeting PDE4 can be used to study PDE4 density and function, and evaluate new PDE4 therapeutics, in vivo in a non-invasive way, as has been shown using the carbon-11 labeled PDE4 inhibitor R-(-)-rolipram. Herein we describe a small series of rolipram analogs that contain fluoro- or iodo-substituents that could be used as fluorine-18 PET or iodine-123 SPECT PDE4 radiotracers. This series was evaluated with an in vitro binding assay and a 4-(fluoromethyl) derivative of rolipram, MNI-617, was identified, with a five-fold increase in affinity for PDE4 (Kd = 0.26 nM) over R-(-)-rolipram (Kd = 1.6 nM). A deutero-analogue d2-[18F]MNI-617 was radiolabeled and produced in 23% yield with high (>5 Ci/μmol) specific activity and evaluated in non-human primate, where it rapidly entered the brain, with SUVs between 4 and 5, and with a distribution pattern consistent with that of PDE4.
Automated synthesis and purification of [18F]fluoro-[di-deutero] methyl tosylate
Beyerlein, Friederike,Piel, Markus,Hoehnemann, Sabine,Roesch, Frank
, p. 360 - 363 (2013/07/26)
Automated synthetic procedures of [18F]fluoro-[di-deutero]methyl tosylate on a GE TRACERlab FX F-N module and a non-commercial synthesis module have been developed. The syntheses included azeotropic drying of the [ 18F]fluoride, nucleophilic 18F-fluorination of bis(tosyloxy)-[di-deutero]methane, HPLC purification and subsequent formulation of the synthesized [18F]fluoro-[di-deutero]methyl tosylate (d 2-[18F]FMT) in organic solvents. Automation shortened the total synthesis time to 50 min, resulting in an average radiochemical yield of about 50% and high radiochemical purity (>98%). The possible application of this procedure to commercially available synthesis modules might be of significance for the production of deuterated 18F-fluoromethylated imaging probes in the future. Copyright
