KF21213 is a highly selective ligand for mapping CNS adenosineA_2Areceptors. KF21213 shows a high affinity for the adenosineA_2Areceptors (K_i=3.0 nM).

Ki: 3.0 nM (A_2Areceptor)^[1]

[¹¹C]KF21213 as a PET ligand for mapping adenosine A_2Areceptors in the central nervous system (CNS). KF21213 shows a high affinity for the adenosine A_2Areceptors in vitro (K_i=3.0 nM) and a very low affinity for the A₁receptors (K_i>10,000 nM)^[1].

The uptake of [¹¹C]KF21213 by the striatum gradually increases for the first 15 min and then decreases. The uptake by the cortex and cerebellum is rapidly decreased after injection. Their levels are compatible with that in the blood. Consequently, the uptake ratios of striatum to cortex and striatum to cerebellum increases up to 8.6±1.6 and 10.5±2.1 (N=4), respectively, by 60 min. The striatal activity level of [¹¹C]KF21213 is retained for the initial 5 min and then gradually decreased with time, whereas that of [¹¹C]KF18446 rapidly decreases.The cerebellar activity of the two ligands rapidly decreases.The striatum-to-cerebellum uptake ratio for [¹¹C]KF21213 gradually increases to 2.4 6 0.5 (N 5 3) by 50-60 min, whereas that for [¹¹C]KF18446 increases for the first 10 min and remains constant (1.4±0.3, N=3, at 25-35 min)^[1].

354.40

C₁₉H₂₂N₄O₃

155271-17-3

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