1092351-10-4

PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM[1].

PSB-603 is an adenosine receptor A2b antagonist (IC50 = 1.13 nM against 10 μM A2bR agonist NECA-induced calcium response in Jurk at T cells in the presence of 200 nM A2aR antagonist MSX-2) th at targets A2bR with high affinity (KD = 0.403 nM/human0.457 nM/rat4.09 nM/mouse A2bR; Ki against 0.3 nM [3H]PSB-603 = 0.553 nM/human0.355 nM/rat0.265 nM/mouse A2bR) and selectivityexhibiting little affinity toward A1A2aor A3 adenosine receptors by competition binding assay (Ki >10 μM against 0.4 nM [3H]DPCPX for human/r at A1R1 nM [3H]MSX-2 for human/mouse/r at A2aR10 nM [3H]NECA for human/mouse/r at A3R) with the exception of mouse A1R (Ki = 42.2 nM against 0.4 nM [3H]DPCPX).''PSB-603 is known to modify cellular metabolism and enhance cellular sensitivity for chemotherapy. ThusPSB-603 is recognized to possess anticancer actionwhich has been studied in colorectal cancer.

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[1] Thomas Borrmann, et al. 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity. J Med Chem. 2009 Jul 9;52(13):3994-4006. DOI:10.1021/jm900413e
[2] Mohamad Wessam Alnouri, et al. Selectivity is species-dependent: Characterization of standard agonists and antagonists at human, rat, and mouse adenosine receptors. Purinergic Signal. 2015 Sep;11(3):389-407. DOI:10.1007/s11302-015-9460-9
[3] Nadine Borg, et al. CD73 on T Cells Orchestrates Cardiac Wound Healing After Myocardial Infarction by Purinergic Metabolic Reprogramming. Circulation. 2017 Jul 18;136(3):297-313. DOI:10.1161/CIRCULATIONAHA.116.023365
[4] Magdalena Kotańska, et al. PSB 603 - a known selective adenosine A2B receptor antagonist-has anti-inflammatory activity in mice. Biomed Pharmacother. 2021 Mar;135:111164. DOI:10.1016/j.biopha.2020.111164