1996
DOI: 10.1016/s0002-8703(96)90190-8
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Renin inhibition: A novel therapy for cardiovascular disease

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Cited by 15 publications
(6 citation statements)
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“…However, the high specificity of human renin for human angiotensinogen was widely recognized as a significant limitation to the study of DRIs across species, 101 and the early in vivo assessment of human-specific DRIs has required the use of primates. 102 These animals are typically normotensive, and therefore, to detect effects on BP or changes in plasma renin activity (PRA) or total renin concentration, the use of a low sodium diet or diuretic pretreatment to activate the RAS is required. The first DRI to demonstrate BP lowering effects following oral administration was N2-[(phenylmethoxy)carbonyl]-L-arginyl-L-arginyl-L-prolyl-L-phenylalanyl-L-histidyl-(3S,4S)-4-amino-3-hydroxy-6-methylheptanoyl-L-isoleucyl-L-histidyl-N6-[(1,1-dimethylethoxy)carbonyl]-L-lysinemethyl ester (CGP29287).…”
Section: Preclinical Pharmacology Of Direct Renin Inhibitionmentioning
confidence: 99%
“…However, the high specificity of human renin for human angiotensinogen was widely recognized as a significant limitation to the study of DRIs across species, 101 and the early in vivo assessment of human-specific DRIs has required the use of primates. 102 These animals are typically normotensive, and therefore, to detect effects on BP or changes in plasma renin activity (PRA) or total renin concentration, the use of a low sodium diet or diuretic pretreatment to activate the RAS is required. The first DRI to demonstrate BP lowering effects following oral administration was N2-[(phenylmethoxy)carbonyl]-L-arginyl-L-arginyl-L-prolyl-L-phenylalanyl-L-histidyl-(3S,4S)-4-amino-3-hydroxy-6-methylheptanoyl-L-isoleucyl-L-histidyl-N6-[(1,1-dimethylethoxy)carbonyl]-L-lysinemethyl ester (CGP29287).…”
Section: Preclinical Pharmacology Of Direct Renin Inhibitionmentioning
confidence: 99%
“…14 Renin inhibition has potential for therapeutic benefits in conditions associated with high PRA. 11,15 Renin receptors have been identified in the human kidney. 16 In diabetes, the increase in prorenin exceeds substantially the increase in other diseases 17 and prorenin levels in type II diabetes correlate with severity of proteinuria and retinopathy.…”
Section: Potential For Direct Renin Inhibitionmentioning
confidence: 99%
“…The blockade induced by ACE inhibitors may be incomplete. In the cascade it is the renin-angiotensinogen interaction and not the ACE step that is rate limiting [63].…”
Section: Non-ace-dependent Pathwaysmentioning
confidence: 99%