RGNCY-0020 (JNJ-40255293 Adenosine A2AA1 Antagonist)

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Adenosine A2A antagonists may have therapeutic potential in the treatment of Parkinson’s disease.  JNJ-40255293 is a high-affinity (7.5 nM) antagonist at the human A2A receptor with 7-fold in vitro selectivity versus the human A1 receptor. A similar A2A:A1 selectivity was seen in vivo (ED50’s of 0.21 and 2.1 mg/kg p.o. for occupancy of rat brain A2A and A1 receptors, respectively). JNJ-40255293 did not affect dopamine and noradrenaline release in the prefrontal cortex and the striatum. JNJ-40255293 demonstrated remarkable potential in experimental models of PD. However, 1 month in vivo rat studies revealed neurotoxic effects associated with this compound.

Systematic Name: 2-amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno[1,2-d]pyrimidin-5-one

SMILES: NC(N=C1C2=CC=CC=C2)=NC(C3=CC(OCCN4CCOCC4)=CC=C35)=C1C5=O

Molecular Weight: 402.45

Formula: C23H22N4O3