PMID: 3928488Sep 1, 1985Paper

Effects of a specific and long-acting renin inhibitor in the marmoset

Hypertension
J M WoodK G Hofbauer

Abstract

Inhibition of renin was induced in conscious marmosets with CGP 29 287, Z-Arg-Arg-Pro-Phe-His-Sta-Ile-His-Lys (Boc)-OMe, a renin inhibitor with a prolonged duration of action. In vitro, CGP 29 287 is a potent inhibitor of primate plasma renin (inhibitory concentration, 50%: human = 1 X 10(-9) M; marmoset = 5 X 10(-9) M) and less potent against dog (2 X 10(-7) M) or rat (3 X 10(-5) M) plasma renin. CGP 29 287 is a weak inhibitor of other aspartic proteases such as porcine pepsin or bovine cathepsin D (inhibitory concentration, 50% = 4 X 10(-5) M). In furosemide-treated marmosets, CGP 29 287 lowered blood pressure and inhibited plasma renin activity during intravenous infusion and after intravenous bolus injection. The duration of action after intravenous injection was dose dependent and ranged from 1 hour after 0.1 mg/kg to more than 3 hours after 10 mg/kg. High doses of CGP 29 287 (100 mg/kg) were active after oral administration. In all experiments a close relation between inhibition of plasma renin activity and reduction of blood pressure was found. A maximum hypotensive response to CGP 29 287 was associated with complete inhibition of plasma renin activity, and the recovery of blood pressure was accompanied by recovery of pl...Continue Reading

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Citations

Apr 1, 1990·Medicinal Research Reviews·W J Greenlee
Oct 1, 1995·Cardiovascular Drugs and Therapy·H D Kleinert
Sep 15, 1988·Klinische Wochenschrift·K G Hofbauer, J M Wood
Feb 24, 2009·European Journal of Drug Metabolism and Pharmacokinetics·Venkata V Pavan Kumar, Nuggehally R Srinivas
Jan 1, 1994·Pharmacology & Therapeutics·J M WoodJ Maibaum
Jan 1, 1991·Biochimie·S ScharpeG Vriend
Jan 1, 1987·The Journal of Clinical Investigation·D J Campbell
Jun 1, 1987·Proceedings of the National Academy of Sciences of the United States of America·J B MichelJ Ménard
Jan 1, 1987·Journal of Enzyme Inhibition·J M WoodK G Hofbauer
Sep 4, 2008·Expert Opinion on Emerging Drugs·Helmy SiragyDavid C Lieb
Jan 1, 1987·Clinical and Experimental Hypertension. Part A, Theory and Practice·J M WoodK G Hofbauer
Jan 11, 1991·Clinical and Experimental Hypertension. Part A, Theory and Practice·R L PanekD G Taylor
Jan 1, 1987·Clinical and Experimental Hypertension. Part A, Theory and Practice·M de GasparoC Heusser
Jan 1, 1987·Clinical and Experimental Hypertension. Part A, Theory and Practice·J M WoodK G Hofbauer
Sep 1, 1988·The American Journal of the Medical Sciences·R T Talwalkar, T A Kotchen
Mar 1, 1989·American Heart Journal·J B MichelJ Ménard
Jan 1, 1989·British Journal of Clinical Pharmacology·M A SchalekampF H Derkx
May 2, 2015·Phytotherapy Research : PTR·Om P Gulati
Feb 2, 2008·Journal of the American College of Cardiology·Alan H Gradman, Rishi Kad
Oct 24, 2006·Lancet·Jan A StaessenTom Richart
Jul 1, 1990·Hypertension·P CorvolJ Ménard
Dec 1, 1986·Hypertension·D T PalsG A Johnson
Jun 1, 1990·Hypertension·T KokubuP F Salmon
May 1, 1991·Hypertension·M Martinez-Maldonado
Jun 1, 1988·Hypertension·K HiwadaY Iijima
Mar 1, 1988·Hypertension·M M de GasparoC H Heusser
Mar 1, 1992·Hypertension·M VéniantW Fischli
Jun 1, 1989·Hypertension·P F MentoB M Wilkes
Jul 1, 1991·Hypertension·W FischliQ Branca
Jul 28, 1990·BMJ : British Medical Journal·A H van den MeirackerM A Schalekamp
Mar 2, 2006·Journal of Hypertension·Michel AziziNorman K Hollenberg
Dec 1, 1986·Hypertension·E Haber
May 1, 1989·British Journal of Clinical Pharmacology·M de GasparoJ Menard
Dec 19, 2020·Journal of Biomolecular Structure & Dynamics·Sudha Bhagwati, Mohammad Imran Siddiqi

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