Lai, Thu Hang published the artcileDevelopment of 18F-labeled radiotracers for PET imaging of the adenosine A2A receptor: synthesis, radiolabeling and preliminary biological evaluation, Quality Control of 76283-09-5, the publication is International Journal of Molecular Sciences (2021), 22(5), 2285, database is CAplus and MEDLINE.
The adenosine A2A receptor (A2AR) represents a potential therapeutic target for neurodegenerative diseases. Aiming at the development of a positron emission tomog. (PET) radiotracer to monitor changes of receptor d. and/or occupancy during the A2AR-tailored therapy, authors designed a library of fluorinated analogs based on a recently published lead compound (PPY). Among those, the highly affine 4-fluorobenzyl derivate (Ki(hA2AR) = 5.3 nM) and the 2-fluorobenzyl derivate (Ki(hA2AR) = 2.1 nM) were chosen for 18F-labeling via an alc. enhanced copper-mediated procedure starting from the corresponding boronic acid pinacol ester precursors. Investigations of the metabolic stability of compound I (R = p-18F, o-18F) in CD-1 mice by radio-HPLC anal. revealed parent fractions of more than 76% of total activity in the brain. Specific binding of I (R = o-18F)on mice brain slices was demonstrated by in vitro autoradiog. In vivo PET/magnetic resonance imaging (MRI) studies in CD-1 mice revealed a reasonable high initial brain uptake for both radiotracers, followed by a fast clearance.
International Journal of Molecular Sciences published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Quality Control of 76283-09-5.
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