SCH 442416

SCH 442416 is a potent, brain-permeable, and selective adenosine A_2A receptor (A_2AR) antagonist.¹ It is selective for A_2AR with a K_i value of 0.048 nM compared to 1,111, >10,000, and >10,000 nM for A₁R, A_2BR, and A₃R, respectively, using human recombinant protein in a radioligand binding assay. It is also selective for A_2AR (K_i = 0.50 nM) in rat cerebral membranes over A₁R and A₃R (K_is = 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 A_2AR agonist-induced arteriole dilation.²

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1. Todde, S., Moresco, R.M., Simonelli, P., et al. Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A_2A receptor system using positron emission tomography. J. Med. Chem. 43(23), 4359-4362 (2000).

2. Maimon, N., Titus, P.A., and Sarelius, I.H. Pre-exposure to adenosine, acting via A(2A) receptors on endothelial cells, alters the protein kinase A dependence of adenosine-induced dilation in skeletal muscle resistance arterioles. J. Physiol. 52(12), 2575-2590 (2014).