Quinaprilat-d5 是一种 Quinaprilat 氘代物。Quinaprilat 是一种非巯基 ACE 抑制剂,是Quinapril 活性代谢物。Quinaprilat 特异性阻断血管紧张素 I 向血管收缩剂血管紧张素 II 的转化,并抑制缓激肽的降解。Quinaprilat 主要作为血管扩张剂,降低外周和肾血管的总阻力。
生物活性
Quinaprilat-d 5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance[1].
体外研究(In Vitro)
Quinaprilat-d5 (5 μM) mediates the interaction of organic anion transporter 3 (hOAT3) which can promote renal active secretion of quinapril that increases uptake of quinaprilat to 25-fold in HEK293 cells and hOAT3 affinity Km for quinaprilat is 13.4 μM.Quinaprilat-d5 (100 nM, 20 min) can inhibit the activity of protein kinase C (PKC) by activing the B1 receptor resulting in the release of NO in human lung microvascular endothelial (HLMVE) cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Quinaprilat-d5 (oral gavage, 3 mg/kg, every day, 6 days) has some anti-hypertensive effect by combining with other drugs in male spontaneous hypertensive rats (SHRs). has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: