Benazepril-d5 is intended for use as an internal standard for the quantification of benazepril . Benazepril is a prodrug of the angiotensin converting enzyme (ACE) inhibitor benazeprilat .1 It is metabolized to benazeprilat by hepatic esterases. Benazepril inhibits the in vitro enzymatic activity of partially purified ACE isolated from rabbit lung (IC50 = 2 nM).2 It decreases the triglyceride and total cholesterol levels in normotensive rats when administered at a dose of 30 mg/kg and decreases aortic atherosclerosis in cholesterol-fed rabbits when administered at a dose of 3 mg/kg per day.3 Benazepril (0.1-10 mg/kg per day) reduces blood pressure in spontaneously hypertensive rats.4 It also decreases proteinuria in cats with chronic kidney disease when administered at doses ranging from 0.5 to 1 mg/kg per day.5 Formulations containing benazepril have been used to treat hypertension, congestive heart failure, and chronic kidney disease in both human and veterinary medicine.
1.Toutain, P.L., and LefÈbvre, H.P.Pharmacokinetics and pharmacokinetic/pharmacodynamic relationships for angiotensin-converting enzyme inhibitorsJ. Vet. Pharmacol. Ther.27(6)515-525(2004) 2.Ksander, G.M., Erion, M., Yuan, A.M., et al.Dual angiotensin converting enzyme/thromboxane synthase inhibitorsJ. Med. Chem.37(12)1823-1832(1994) 3.Yamamoto, S., Takemori, E., Hasegawa, Y., et al.General pharmacology of the novel angiotensin converting enzyme inhibitor benazepril hydrochloride. Effects on cardiovascular, visceral and renal functions and on hemodynamicsArzneimittelforschung41(9)913-923(1991) 4.Watthey, J.W.H., Stanton, J.L., Desai, M., et al.Synthesis and biological properties of (carboxyalkyl)amino-substituted bicyclic lactam inhibitors of angiotensin converting enzymeJ. Med. Chem.28(10)1511-1516(1985) 5.King, J.N., Gunn-Moore, D.A., Tasker, S., et al.Tolerability and efficacy of benazepril in cats with chronic kidney diseaseJ. Vet. Intern. Med.20(5)1054-1064(2006)