Quinapril hydrochloride (Accupril) is the hydrochloride salt of quinapril that is an angiotensin-converting enzyme inhibitor with a Ki of 20 μM. Quinapril hydrochloride (Accupril) used in the treatment of hypertension and congestive heart failure. Quinapril is a prodrug. Quinapril is converted to its active metabolite, quinaprilat, in the liver. Quinapril inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I. Angiotensin II is a powerful vasoconstrictor and increases blood pressure through a variety of mechanisms. Due to reduced angiotensin production, plasma concentrations of aldosterone are also reduced, resulting in increased excretion of sodium in the urine and increased concentrations of potassium in the blood.
| Molecular Weight | 474.98 |
| Formula | C25H30N2O5.HCl |
| CAS Number | 82586-55-8 |
| Solubility (25°C) | Water 90 mg/mL Ethanol 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Beata Stanisz. The influence of pharmaceutical excipients on quinapril hydrochloride stability
[4] H R Kaplan, et al. Quinapril: overview of preclinical data
[5] D Canter, et al. The safety profile of quinapril: is there a difference among ACE inhibitors?
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