A2AAR antagonist 5 

A2AAR antagonist 5 is a selective A_2AAR antagonist. A2AAR antagonist 5 inhibits NECA-stimulated adenylyl cyclase activity in hA_2AAR-expressing CHO cells with an IC₅₀ value of 1863 nM. A2AAR antagonist 5 possesses strong free radical scavenging activity, with an EC₅₀ value of 22.21 μM in the DPPH assay. A2AAR antagonist 5 exerts notable neuroprotective effects in in vitro cerebral ischemia models. A2AAR antagonist 5 can be used for the study of cerebral ischemia^[1].

A2AAR antagonist 5 (Compound 3) exhibits potent affinity for hA_2A adenosine receptor with a K_i value of 57 nM, shows no affinity for hA₁ adenosine receptor (K_i > 30,000 nM), has moderate affinity for hA₃ adenosine receptor (K_i = 358 nM), and no activity on hA_2B adenosine receptor (IC₅₀ > 30,000 nM)^[1].
A2AAR antagonist 5 exerts antagonistic activity against hA_2A adenosine receptor in CHO cells expressing hA_2A , with an IC₅₀ value of 1416 nM for inhibiting NECA-stimulated adenylyl cyclase activity^[1].
A2AAR antagonist 5 displays potent free radical scavenging activity, with an EC₅₀ value of 22.21 μM^[1].
A2AAR antagonist 5 (200 nM, administered 15 min before, during Oxygen-Glucose Deprivation (OGD), and 5 min after OGD significantly delays the onset of anoxic depolarization (AD) induced by oxygen-glucose deprivation (OGD) in the CA1 region tested in acute rat hippocampal slices^[1].
A2AAR antagonist 5 (1-10 μM, administered during 30 min OGD and subsequent 24 h recovery) exerts significant neuroprotective effects, reducing OGD-induced neuronal damage in the CA1 subfield tested in rat organotypic hippocampal slices ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

456.46

C₂₃H₂₀N₈O₃

O=C(NC1=CC=C(C2=CN3C(C(N)=N2)=NN(C4=CC=CC=C4)C3=O)C=C1)CN5N=C(C)CC5=O

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• [1]. Calenda S, et al. 8-Amino-1,2,4-triazolo[4,3-a]pyrazin-3-one derivatives hybridized with antioxidants: new highly potent and selective human A2A adenosine receptor antagonists as useful agents against cerebral ischemia. Bioorg Chem. 2025 Sep;164:108855.  [Content Brief]