RGNCY-0020 (JNJ-40255293 Adenosine A2AA1 Antagonist)
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
Molecular Weight: 402.45
Reference: Atack, John R., et al. "JNJ-40255293, a Novel Adenosine A2A/A1 Antagonist with Efficacy in Preclinical Models of Parkinson’s Disease." ACS Chemical Neuroscience 5.10 (2014): 1005-1019.
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Tags: Adenosine, Parkinson's, RGNCY-0020, JNJ, JNJ-40255293, A2AA1, Parkinson, Parkinsons, A2A