This Article Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Request Permissions Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Cumin, F. Articles by Graf, P. Search for Related Content PubMed PubMed Citation Articles by Cumin, F. Articles by Graf, P.

Hypertension, Vol 14, 379-384, Copyright © 1989 by American Heart Association

ARTICLES

Assays to measure nanomolar levels of the renin inhibitor CGP 38 560 in plasma

F Cumin, M de Gasparo, JM Wood, C Schnell, F Frueh and P Graf
Biological Research Department, Ciba-Geigy Limited, Basel, Switzerland.

A radioinhibitor binding assay and an enzyme inhibition assay have been developed to measure plasma levels of CGP 38 560, a potent human renin inhibitor. The detection limit of the assays was between 0.5 and 1 pmol/ml. There was a good correlation (r = 0.989) between the two assays for the measurement of human plasma spiked with CGP 38 560 in concentrations from 1.9 nM to 12 microM. Intra-assay variability was 6.1-17.3% and 4.4-27.2% for the radioinhibitor binding assay and the enzyme inhibition assay, respectively. Interassay variability was 6.0- 28.2% and 3.8-28.4% for the radioinhibitor binding assay and the enzyme inhibition assay, respectively. Blood samples were collected during a pharmacological study performed in normotensive human volunteers on an unrestricted diet who were infused during a 30-minute period with CGP 38 560 A (50 micrograms/kg). Similar values for the concentrations of renin inhibitor in plasma were obtained with the radioinhibitor binding assay and the enzyme inhibitor assay, and there was a significant correlation between values obtained with the two different methodologies (r = 0.94). The plasma levels of renin inhibitor reached a maximum at the end of infusion and then decreased rapidly, indicating a short plasma half-life. The changes in biochemical parameters, plasma renin activity, and plasma concentration of active renin could be related to the concentrations of CGP 38 560 measured in the plasma.

This article has been cited by other articles:

				P. van Paassen, D. de Zeeuw, G. Navis, and P. E. de Jong Renal and systemic effects of continued treatment with renin inhibitor remikiren in hypertensive patients with normal and impaired renal function Nephrol. Dial. Transplant., May 1, 2000; 15(5): 637 - 643. [Abstract] [Full Text] [PDF]

				J. Menard, R. S. Boger, D. M. Moyse, T. T. Guyene, H. N. Glassman, and H. D. Kleinert Dose-Dependent Effects of the Renin Inhibitor Zankiren HCl After a Single Oral Dose in Mildly Sodium-Depleted Normotensive Subjects Circulation, January 15, 1995; 91(2): 330 - 338. [Abstract] [Full Text]