CP-71,362 - A PENTAPEPTIDE RENIN INHIBITOR SELECTIVE FOR THE CANINE ENZYME

Authors
MANGIAPANE ML MACANDREW JT ELLERY SS SMITH AH PURCELL IM KLEINMAN EF HOLT WF MURPHY WR
Citation
Ml. Mangiapane et al., CP-71,362 - A PENTAPEPTIDE RENIN INHIBITOR SELECTIVE FOR THE CANINE ENZYME, Clinical and experimental hypertension, 16(4), 1994, pp. 507-533
Citations number
23
Categorie Soggetti
Pharmacology & Pharmacy","Cardiac & Cardiovascular System
Journal title
Clinical and experimental hypertension → ACNP
ISSN journal
10641963
Volume
16
Issue
4
Year of publication
1994
Pages
507 - 533
Database
ISI
SICI code
1064-1963(1994)16:4<507:C-APRI>2.0.ZU;2-N
Abstract
Most renin inhibitors are primate-specific. In the present paper, we d escribe the effects of CP-71,362, a pentapeptide which preferentially inhibits canine (and to a lesser extent, rat) plasma renin. Vs. the ca nine enzyme, its affinity (IC50 = 3.3 x 10(-12) M) is 1000x greater th an for rat renin (IC50 = 3.3 x 10(-9) M), and 10000x greater than for human (IC50 = 2.3 x 10(-8) M), cynomolgus monkey (IC50 = 1.6 x 10(-8) M), or guinea pig (IC50 = 5.2 x 10(-8) M) enzyme.