human a3 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。

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

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。

CHEMBL241987 靶向腺苷受体 A3（人）。

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。

HEMADO is a potent and selective agonist of adenosine A3 receptor (Ki: 1.1 nM at the human A3 subtype).

LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).

MRS-1191 is an effective and selective A3 adenosine receptor antagonist (KB: 92 nM, a Ki: 31.4 nM for human A3 receptor and an IC50: 120 nM for CHO cells).

MRS1177 is an effective and selective antagonist of the human Adenosine A3 receptor (hA3AR) (Ki: 0.3 nM).

MRS1186 is an effective and selective antagonist of the human Adenosine A3 receptor (Ki: 7.66 nM).

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。

A3AR antagonist 5 (Compound 16) 作为人类腺苷 A3 受体的选择性拮抗剂，展现出亲和力pC 4.542 μM。

MRS1220 是一种高效、选择性的人 A3 腺苷受体 (hA3AR) 拮抗剂，Ki 为 0.59 nM，可用于中枢神经系统疾病的研究。MRS1220 在体内还减少了胶质母细胞瘤的肿瘤大小和血管形成。

antagonist for the human adenosine A3 receptor

PSB-10 hydrochloride is a human adenosine A3 receptor antagonist.

PSB 11 hydrochloride is a human adenosine A3 receptor antagonist.

VUF 5574 是一种选择性的 腺苷A3 受体拮抗剂，对重组人受体的Ki 为 4.03 nM。

CP-608039 is a selective adenosine A3 receptor agonist for both human A3 and human A1 receptors.

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.

hA3AR agonist 1 是一种有效的人腺苷受体（hA3AR）激动剂 (Ki = 2.40 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。

A1/A3 AR antagonist 1 (compound 10) 是一种有效的、双重腺苷酸 1 (A1)和腺苷酸 3 (A3)受体拮抗剂，能够作用于人 A1 (Ki: 37.6 nM)、人 A3 (Ki: 25.4 nM) 和大鼠 A1 (Ki: 1.47 nM)。A1/A3 AR antagonist 1 能够用于研究肾衰竭、炎症性肺部疾病和阿尔茨海默症。

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。