Zhou, Xiaoyun published the artcileIn vivo evaluation of [11C]preladenant positron emission tomography for quantification of adenosine A2A receptors in the rat brain, Safety of 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, the publication is Journal of Cerebral Blood Flow & Metabolism (2017), 37(2), 577-589, database is CAplus and MEDLINE.
[11C]Preladenant was developed as a novel adenosine A2A receptor positron emission tomog. radioligand. The present study aims to evaluate the suitability of [11C]preladenant positron emission tomog. for the quantification of striatal A2A receptor d. and the assessment of striatal A2A receptor occupancy by KW-6002. Tracer kinetics was quantified by the two-tissue compartment model, Logan graphical anal. and several reference tissue-based models. Test-retest reproducibility was assessed by repeated imaging on two consecutive days. Two-tissue compartment model and Logan plot estimated comparable distribution volume (VT) values of ∼10 in the A2A receptor-rich striatum and substantially lower values in all extra-striatal regions (∼1.5-2.5). The simplified reference tissue model with midbrain or occipital cortex as the reference region proved to be the best non-invasive model for quantification of A2A receptor, showing a striatal binding potential (BPND) value of ∼5.5, and a test-retest variability of ∼5.5%. The brain metabolite anal. showed that at 60-min post injection, 17% of the radioactivity in the brain was due to radioactive metabolites. The ED50 of KW-6002 in rat striatum for i.p. injection was 0.044-0.062 mg/kg. The study demonstrates that [11C]preladenant is a suitable tracer to quantify striatal A2A receptor d. and assess A2A receptor occupancy by A2A receptor-targeting mols.
Journal of Cerebral Blood Flow & Metabolism published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C10H10O2, Safety of 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine.
Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics