产品
编 号:F315724
分子式:C15H18N8O5
分子量:390.35
产品类型
结构图
CAS No: 313348-27-5
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生物活性:
Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS.
体内研究:
Regadenoson (0.1、0.175、0.25、0.5、1.0、2.5、5 μg/kg;piv;单次) 在清醒的狗中以剂量依赖性方式增加冠状动脉血流量 (CBF) 并降低平均冠状动脉阻力。 Regadenoson (2.5 μg/kg;piv;30 秒内单次) 增加清醒犬的冠状动脉血流。 Regadenoson (0.5 μg/kg;iv;单次;替莫唑胺给药后 60 或 90 分钟) 促进替莫唑胺向大鼠 CNS 的递送。Animal Model:Mongrel dogs (23-27 kg)
Dosage:0.1, 0.175, 0.25, 0.5, 1.0, 2.5, 5 μg/kg
Administration:Peripheral intravenous injection; single.
Result:Increased mean CBF (coronary blood flow) in a dose-dependent manner, with an ED50 of 0.34 μg/kg and resulted in a maximal increase of 154 mL/min from baseline (45 mL/min).Caused a dose-dependent decrease in mean coronary resistance with a maximal decrease of 73 and 75 % at 2.5 and 5 μg/kg, respectively.
Animal Model:Mongrel dogs (23-27 kg)
Dosage:2.5 μg/kg
Administration:Peripheral intravenous injection; single in 30 s.
Result:Reached 84% of the peak reactive hyperemia flow following a 20-s-long coronary occlusion (201 mL/min).
Animal Model:Female F344 rats (150-170 g)
Dosage:0.5 μg/kg
Administration:Intravenous injection; single (60 or 90 min after Temozolomide administration)
Result:Increaseed levels of Temozolomide by 60 % in normal brain without affecting plasma concentrations.