a2b receptor antagonist 1

A2B receptor antagonist 1 是一个有效的 A2B 腺苷受体 (A2B adenosine receptor) 拮抗剂。

GS-6201 (CVT-6883) 是选择性腺苷 A2B 受体拮抗剂。它对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。它降低了小鼠急性心肌梗死后心脏中 caspase-1 的活性，并减弱了心脏重塑。它减弱了致敏小鼠 NECA，AMP 或变应原诱导的气道反应性。

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].

Adenosine receptor antagonist 2 是一种具有口服活性的 A2a (IC50: 1 nM) A2b (IC50: 3 nM) 腺苷受体拮抗剂。Adenosine receptor antagonist 2 表现出抗肿瘤效果。

PSB-1115 potassium salt是选择性A2B腺苷受体拮抗剂，能够抑制三硝基苯磺酸(TNBS)诱导的乙酰胆碱(ACh)收缩抑制现象。