产品
编 号:F385465
分子式:C25H18ClN5O2S2
分子量:520.03
产品类型
结构图
CAS No: 544417-40-5
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产品详情
生物活性:
Capadenoson is a selective agonist of adenosine-A1 receptor.
体内研究:
In the in vivo experiments, Wistar rats and SHR are pre-treated with Capadenoson at a concentration of 0.15 mg/kg for 5 days. On day 5, a stress test (physical restraint) is performed for 2 hours. The plasma concentration of Capadenoson measured 3 hours after drug intake remains constant in the 5 days prior to the restraint stress test and averaged 7.63 μg/L on day 4 and 5, respectively.
体外研究:
To further elucidate the pharmacological properties of Capadenson, GTP shift assays are performed with the standard full A1-agonist CCPA and the A1-antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX). CCPA shows a Ki value of 4.2 nM in the binding assay on rat cortical brain membranes. In the presence of 1 mM GTP this Ki value shifts to a value of 64 nM. Therefore the GTP shift for CCPA is 15. DPCPX shows a GTP shift of 1 with virtually identical Ki values in the absence and presence of GTP. Capadenson shows a Ki value of 24 nM in the binding assay. In the presence of 1 mM GTP this Ki value shifts to a value of 116 nM resulting in a GTP shift of 5 for Capadenoson.