产品
编 号：F108212
分子式：C23H21D5N2O5
分子量：415.49
分子式：C23H21D5N2O5
分子量：415.49
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CAS No: 1279034-23-9
产品详情
生物活性：
Quinaprilat-d5 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.
体内研究：
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).Animal Model:Male spontaneous hypertensive rats (SHRs) (230-250 g)
Dosage:3 mg/kg
Administration:Oral gavage; every day; 6 days
Result:Caused a significant drop in blood pressure from day 1 to day 5 by combining quinapril and gemcabene while each alone had no effect. Decreased plasma concentration of quinaprilat on the fifth day.
Animal Model:
Dosage:
Administration:
Result:Result: The pharmacokinetic parameters of quinaprilat Parameter
AUC(0-24 h)4.62 μM/h
Ae(0-24 h)23.1 μg
renal clearance31.0 mL/h
体外研究：
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.
Quinaprilat-d5 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.
体内研究：
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).Animal Model:Male spontaneous hypertensive rats (SHRs) (230-250 g)
Dosage:3 mg/kg
Administration:Oral gavage; every day; 6 days
Result:Caused a significant drop in blood pressure from day 1 to day 5 by combining quinapril and gemcabene while each alone had no effect. Decreased plasma concentration of quinaprilat on the fifth day.
Animal Model:
Dosage:
Administration:
Result:Result: The pharmacokinetic parameters of quinaprilat Parameter
AUC(0-24 h)4.62 μM/h
Ae(0-24 h)23.1 μg
renal clearance31.0 mL/h
体外研究：
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.
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