产品
编 号:F341174
分子式:C13H13N5O2
分子量:271.27
产品类型
结构图
CAS No: 37762-06-4
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产品详情
生物活性:
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
体内研究:
Zaprinast (3 和 10 mg/kg;腹腔注射) 可增强高架十字迷宫 (EPM) 中的空间记忆,并减少 Hughes 盒测试中的探索活动。 Animal Model:Male inbred BALB/c ByJ mice aged 7 weeks
Dosage:3 and 10 mg/kg
Administration:IP; 60 min before the first session
Result:Significantly decreased second-day latency compared to the control group in the EPM test with 10 mg/kg. Significantly shortened the time spent in the novel side in the Hughes box with 10 mg/kg.
体外研究:
Zaprinast (0.1, 0.3, 1, 3, 10, 30 μM) 在 HEK293 细胞中以浓度依赖性方式诱导共表达 FLAG-hGPR35 和四种外源 Gα 蛋白的转染子中的细胞内钙动员。 Zaprinast (100 μM;5 分钟) 可促进 HEK293T 细胞中人 GPR35a C 末端尾部 5 个不同氨基酸的磷酸化。