MW 345.4 Da, Purity >99%. Potent, highly selective A2A receptor antagonist. (Ki values are 1-2, 289 and >10000 nM at A2A, A1 and A3 receptors, respectively). Displays therapeutic effects in animal Parkinson's models and elicits locomotor sensitization *in vivo*.
View Alternative Names
A1AR, A1R, A2AAR, A2aR, A3AR, A3R, AA1R_HUMAN, AA2AR_HUMAN, AA2BR_HUMAN, AA3R_HUMAN, AD 026, ADENO, ADORA 1, ADORA 2, ADORA 3, ADORA2A, ARA3, Adenosine A2 receptor, Adenosine A2a receptor, Adenosine A3 receptor, Adenosine receptor A1, Adenosine receptor A2a, Adenosine receptor A2b, Adenosine receptor A3, Adenosine receptor subtype A2a, GPCR 2, HGNC:264, Netrin 1 receptor, RDC 7, RDC 8, RP11 552M11.7, Ri, TGPCR1, adora 2b, bA552M11.5, hA2aR
- Chemical Structure
Lab
Chemical Structure - SCH-58261, A2A antagonist (AB120439)
2D chemical structure image of ab120439, SCH-58261, A2Aantagonist
Properties and storage information
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Storage information
Supplementary information
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Biological function summary
These receptors modulate a wide array of physiological functions. As parts of receptor complexes they influence neurotransmission inflammation and immune responses. Specifically adenosine acts through these receptors to inhibit neurotransmitter release in the brain providing a neuroprotective effect under stress conditions. Adenosine A2a Receptor is known to play a role in vasodilation and immune cell regulation while A3AR has implications in both cardioprotection and cancer biology. These receptors function collectively and independently facilitating cellular communication and maintaining homeostasis.
Pathways
These receptors engage in important signaling cascades such as the cyclic AMP (cAMP) pathway where they either inhibit or stimulate cAMP production through different G proteins. They also participate in MAPK and PI3K/Akt pathways which are critical for cell survival and proliferation. Adenosine Receptor A2a is often studied in relation to dopamine D2 receptors highlighting its role in neuromodulation and potential therapeutic targets for neurological disorders.
Publications (3)
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Cell death discovery 8:475 PubMed36456564
2022
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Theranostics 8:5713-5730 PubMed30555576
2018
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PloS one 10:e0134488 PubMed26252389
2015
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