human a2a receptor

MRS-1706 是一种选择性A2B 腺苷受体的反向激动剂，对人 A2B、A2A、A1和 A3受体的Ki 值分别为 1.39、112、157 和 230 nM。

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。

XU1（Benzo[c][1,8]naphthyridin-6(5h)-One） 是一种 Aurora 蛋白激酶抑制剂，用于治疗适合激酶信号转导抑制、调节或调节的疾病。

ANR94 是一种有效的、选择性的腺苷 A2A 受体 (AA2AR) 拮抗剂，对 hAA2AR 的Ki 值为 46 nM。ANR94 具有用于帕金森病的研究潜力。

Tozadenant (SYN115) 是 A2A 腺苷受体拮抗剂，对人和恒河猴的 Ki 分别为 11.5 和 6 nM。

Sch412348 is a potent competitive the human adenosine A2A receptor antagonist with Ki of 0.6 nM and has >1000-fold selectivity over all other adenosine receptors.

CGS 15943 是一种可口服的非黄嘌呤腺苷受体拮抗剂。在转染的 CHO 细胞中，其对人 A1、A2A、A2B 和 A3 腺苷受体的 Ki 分别为 3.5、4.2、16 和 50 nM。

MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 n

N6-Cyclopentyladenosine (CPA) 是一个选择性的腺苷A1 受体 (Adenosine A1 receptor)的激动剂，可用于模拟腺苷A1受体的作用，对人A1、A2A 和 A3 受体的Ki 分别为 2.3 nM、790 nM 和 43 nM。N6-Cyclopentyladenosine (CPA) 可用于调节细胞信号传导、神经递质释放和其他生物学过程。

A2AAR antagonist 4 是一种口服有效的A2A腺苷受体 (A2A Adenosine receptor) 拮抗剂，在人A2AAR上的Ki值为0.36 nM，KB值为1 nM。在10 μM浓度下，它能够完全抑制人A2AAR和人A2bAR。A2AAR antagonist 4 可用于癌症研究，如MC38肿瘤。

A2AAR antagonist 5 是一种选择性的A2AAR拮抗剂，能够抑制在hA2AAR表达的CHO细胞中由NECA刺激引起的腺苷酸环化酶活性，其IC50值为1863 nM。在DPPH实验中，A2AAR antagonist 5 显示出较强的清除自由基活性，EC50值为22.21 μM。在体外脑缺血模型中，该化合物表现出显著的神经保护作用，适用于脑缺血研究。

SCH442416 (SCH 442416) 是选择性和可透过血脑屏障的腺苷A2A 受体拮抗剂，对人和大鼠 A2AR 的Ki 值分别为 0.048 和 0.5 nM，可用于在大鼠和灵长类动物大脑中对腺苷 A2A 受体成像。

MRS3558 is an agonist of A3 adenosine receptors.

CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human). It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 μM) and MAO-A (IC50 ≥ 10 μM). At 1-20 μM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson's disease. An additional strategy in the treatment of Parkinson's disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.

The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively. CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells. However, no dedifferentiation effects or any connection between A3 AR antagonism and dedifferentiation have been demonstrated.

A1AR antagonist 6 (化合物 15) 是 A1 腺苷受体(A1AR)的有效的选择性拮抗剂，其pKi 值为 7.13，pIC50值为 6.38。

A1AR antagonist 5 (化合物 20) 是A1 腺苷受体(A1AR)的有效选择性拮抗剂，其pKi 值为 6.11，pIC50值为 5.83。

A1AR antagonist 4 (compound 22) is a highly developed chemical compound that acts as a potent and selective antagonist of the A1 adenosine receptor (A1AR). It possesses a pIC50 value of 5.51 and a pKi value of 6.29 [1].

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 inhibitor 2 (compound 14b) 是有效的AR(腺苷受体)抑制剂。Adenosine receptor inhibitor 2 显示对 A1/A2AARs 的双重亲和性，对 A1- 的亲和性比A2AAR 更高。Adenosine receptor inhibitor 2 抑制A1AR 和A2AAR 的Ki 分别为 52.2 和 167 nM。

A2AAR/HDAC-IN-1 (compound 14c) 是一种口服具有活力的、平衡的 A2AAR/HDAC 双抑制剂，作用于 A2AAR (Ki: 163.5 nM)、HDAC1 (IC50: 145.3 nM)。A2AAR/HDAC-IN-1 具有抗癌 (anticancer) 效果。

hA2A/hCA XII modulator 1 是 hA2A 腺苷受体 (hA2AAR) 的有效拮抗剂，是一种三唑并吡嗪， 能够作用于hA2AAR (Ki: 6.4 nM)、hA1AR (Ki: 4.819 μM)、hA3AR (Ki>30 μM)。hA2A/hCA XII modulator 1 也人碳酸酐酶 XII (hCA XII) 的有效抑制剂，能够作用于 hCA XII (Ki: 6.2 nM)、hCA II (Ki: 46 nM)、hCA IX (Ki: 466 nM) 和 hCA I (Ki: 8.351 μM)。hA2A/hCA XII modulator 1 表现出研究癌症的潜力。

A2A/A3 AR antagonist-1 (化合物 23) 是一种双重 A2A/A3adenosine receptor(AR)荧光配体，对 hA2AAR 和 hA3AR 的 Ki 值分别为 90 nM 和 31.8 nM。

PSB 0777 ammonium hydrate 是一种选择性腺苷A2A受体激动剂，Ki值对大鼠A2A受体为44.4 nM，对人A2A受体为360 nM。对大鼠A1受体的Ki值≥10000 nM，对人A1受体为541 nM。该化合物大脑渗透性和口服生物利用度较差，但显示在炎性肠病（IBS）研究中的应用潜力。