Benazepril-d5 (hydrochloride) (Synonyms: CGS 14824A-d5)

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)