Pivalopril

• CAT Number: I013475
• CAS Number: 81045-50-3
• Molecular Formula: C16H27NO4S
• Molecular Weight: 329.45
• Purity: ≥95%
• Synonyms: 2-[cyclopentyl-[(2S)-3-(2,2-dimethylpropanoylsulfanyl)-2-methylpropanoyl]amino]acetic acid
• InChI: InChI=1S/C16H27NO4S/c1-11(10-22-15(21)16(2,3)4)14(20)17(9-13(18)19)12-7-5-6-8-12/h11-12H,5-10H2,1-4H3,(H,18,19)/t11-/m1/s1
• InChIKey: XRKXJJYSKUIIEN-LLVKDONJSA-N
• SMILES: CC(CSC(=O)C(C)(C)C)C(=O)N(CC(=O)O)C1CCCC1

Pivalopril is a new orally active angiotensin converting enzyme (ACE) inhibitor.
Pivalopril is a new compound with a hindered sulfur group that has been compared to Captopril for oral angiotensin-converting enzyme (ACE) inhibition in rats and dogs and antihypertensive activity in rats. In separate groups of conscious normotensive rats, Pivalopril (0.03-1.0 mg/kg, orally [p.o.]) produces a dose-related antagonism of angiotensin I (AngI)-induced pressor effects. The ED50 for Pivalopril and Captopril is 0.1 mg/kg. In conscious normotensive dogs, Pivalopril (incremental doses of 0.01-1.0 mg/kg, p.o.) produces a dose-related antagonism of AngI pressor effects. The ED50 is 0.17 mg/kg for Pivalopril and 0.06 mg/kg for Captopril. At equieffective doses the two compounds have similar durations of action. In sodium-deficient, conscious spontaneously hypertensive rats (SHR), Pivalopril (1-100 mg/kg, p.o.) produces a dose-related reduction in mean arterial pressure. The potency and duration are similar to those of Captopril. In the sodium-replete SHR, 5 days of oral dosing with Pivalopril (100 mg/kg per day) decreases mean arterial pressure more effectively than Captopril (100 mg/kg per day). It is concluded that Pivalopril is a potent, orally effective ACE inhibitor and antihypertensive agent[2].

Reference

[1]. Burnier M, et al. RHC 3659: a new orally active angiotensin converting enzyme inhibitor in normal volunteers. Br J Clin Pharmacol. 1981 Dec;12(6):893-9.
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[2]. Wolf PS, et al. Angiotensin-converting enzyme inhibitory and antihypertensive activities of pivalopril (RHC 3659-(S)). Fed Proc. 1984 Apr;43(5):1322-5.
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