pepstatin and ditekiren

pepstatin has been researched along with ditekiren* in 1 studies

Other Studies

1 other study(ies) available for pepstatin and ditekiren

Article	Year
Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo. Journal of medicinal chemistry, 1986, Volume: 29, Issue:10 A structure-activity analysis of peptides containing backbone C alpha-methyl and N alpha-methyl modifications led to the discovery of potent renin inhibitors with high metabolic stability. In vitro, Boc-Pro-Phe-N alpha-MeHis-Leu psi-[CHOHCH2]Val-Ile-Amp (XII) is a potent inhibitor of human plasma renin with IC50 of 0.26 nM. It is a much weaker inhibitor of other aspartic proteases such as porcine pepsin or bovine cathepsin D (IC50 = 6 microM). It was shown not to be degraded by a rat liver homogenate preparation. In vivo, it inhibited plasma renin activity and lowered blood pressure of furosemide-treated cynomolgus monkeys. At a dose of 5 mg/kg iv, the pronounced hypotensive response persisted for greater than 3 h postinfusion. Topics: Animals; Antihypertensive Agents; Drug Stability; Humans; Macaca fascicularis; Male; Oligopeptides; Peptides; Protease Inhibitors; Rats; Rats, Inbred Strains; Renin; Structure-Activity Relationship; Time Factors	1986

Article

Year

Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo.

Journal of medicinal chemistry, 1986, Volume: 29, Issue:10

A structure-activity analysis of peptides containing backbone C alpha-methyl and N alpha-methyl modifications led to the discovery of potent renin inhibitors with high metabolic stability. In vitro, Boc-Pro-Phe-N alpha-MeHis-Leu psi-[CHOHCH2]Val-Ile-Amp (XII) is a potent inhibitor of human plasma renin with IC50 of 0.26 nM. It is a much weaker inhibitor of other aspartic proteases such as porcine pepsin or bovine cathepsin D (IC50 = 6 microM). It was shown not to be degraded by a rat liver homogenate preparation. In vivo, it inhibited plasma renin activity and lowered blood pressure of furosemide-treated cynomolgus monkeys. At a dose of 5 mg/kg iv, the pronounced hypotensive response persisted for greater than 3 h postinfusion.

Topics: Animals; Antihypertensive Agents; Drug Stability; Humans; Macaca fascicularis; Male; Oligopeptides; Peptides; Protease Inhibitors; Rats; Rats, Inbred Strains; Renin; Structure-Activity Relationship; Time Factors

1986