生物活性 | |||
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描述 | Adenosine receptors are a family of GPCRs containing four subtypes (A1 , A2A , A2B and A3 receptors), all of which bind the ubiquitous nucleoside adenosine.[1]. Adenosine is a potent regulator of inflammation. Adenosine mediates its effects on inflammatory cells by engaging one or more cell-surface receptors[2]. SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively[3]. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). It can be used for imaging of adenosine A2A receptors in rat and primate brain[4]. SCH-442416 (0.017 mg/kg; i.p.) completely abrogates the CGS-21680-induced decrease in skeletal muscle injury[5]. SCH442416 (1 μM) significantly attenuates the adenosine-induced dilation (from 15.3 to 5.6 μm)[6]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00531193 | Healthy | Phase 1 | Completed | - | United Kingdom ... 展开 >> Research Site London, United Kingdom 收起 << |
NCT02764892 | Parkinson's Disease | Phase 1 | Completed | - | - |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.57mL 0.51mL 0.26mL |
12.84mL 2.57mL 1.28mL |
25.68mL 5.14mL 2.57mL |
参考文献 |
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