Formulation: A crystalline solid
Formal Name: 2-(2-furanyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine
Purity: ≥98%
Formula Markup: C20H19N7O2
Formula Weight: 389,4
Shelf life (days): 1460
CAS Number: 316173-57-6
Notes: SCH 442416 is a potent, brain-permeable, and selective adenosine A2A receptor (A2AR) antagonist.{40048} It is selective for A2AR with a Ki value of 0.048 nM compared to 1,111, >10,000, and >10,000 nM for A1R, A2BR, and A3R, respectively, using human recombinant protein in a radioligand binding assay. It is also selective for A2AR (Ki = 0.50 nM) in rat cerebral membranes over A1R and A3R (Kis = 1,815 and >10,000, respectively). Biodistribution in rats demonstrates preferential uptake by liver, adrenal gland, kidney, and lungs, and by the striatum in the brain. SCH 442416 (10 μM) attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation.{40049}