a1ar

MIPS521 ({2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone) 是腺苷受体 (A1AR) 的正向变构调节剂，通过调节大鼠脊髓中内源性腺苷水平的升高，在体内表现出减轻疼痛的作用。

A1AR antagonist 2 (compound 18h) 是 A1腺苷受体 (A1 adenosine receptor) 的有效的选择性拮抗剂。A1AR antagonist 2对于 hA1, hA2A，hA2B 的Ki 值分别为 1.49、10.2 和 50.1 nM。

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 1 (compound 18g) 是A1腺苷受体的选择性拮抗剂。A1AR antagonist 1对 hA1, hA2A，hA2B 受体的Ki 值分别为 2.08、6.91 和 31.2 nM。

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].

A1AR antagonist 3 (compound 13) 是一种选择性的腺苷酸 1 (A1) 受体拮抗剂，作用于人 A1 (Ki: 9.69 nM) 和大鼠 A1 (Ki: 0.529 nM)。A1AR antagonist 3 能够用于研究神经性疾病。

N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine) 是一种腺苷衍生物和腺苷受体激动剂，对大鼠和人 A1 的 Ki 值分别为 11.8 nM 和 30.1 nM。

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。

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.

A2A A1 AR antagonist-1 (compound 1a) 具有用于缺血性卒中研究的潜力，它是 A2A A1AR 的双重拮抗剂，Ki 值分别为 5.58 和 24.2 nM。

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。

A2AAR HDAC-IN-2 是一种有效的 A2AAR HDAC 双重抑制剂。A2AAR HDAC-IN-2 对 A2AAR 表现出良好的亲和力 (Ki:10.3 nM), 能够良好的抑制 HDAC1 (IC50:18.5 nM). A2AAR HDAC-IN-2 能够用于研究抗肿瘤。

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。

N6-Ethyladenosine 是腺苷衍生物，是一种腺苷受体激动剂，对 hA1AR 和 hA3AR 的 Ki 值分别为 4.9 和 4.7 nM。

2'-MeCCPA 是一种具有有效性和高选择性的 A1 腺苷受体 (A1AR) 激动剂，对 AR 的 K 值为 1.8 nM。2'-MeCCPA 抑制毛喉素刺激的腺苷酸环化酶活性，IC值为13.1 nM。2'-MeCCPA 具有镇痛活性，可用于研究 HCV 。

FSCPX是一种针对A1 腺苷受体（A1AR）的强效、选择性不可逆拮抗剂，显示出低纳摩尔级的结合效能。此外，FSCPX能有效降低豚鼠心房中的间质腺苷水平，进而改变核苷转运抑制剂NBTI的效果。

CPFPX is a highly selective radioactive ligand for the A1 adenosine receptor (A1AR).

VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.