Remikiren

from Wikipedia, the free encyclopedia
Structural formula
Structure of remikiren
General
Non-proprietary name Remikiren
other names
  • RO-42-5892
  • Remikirenum ( Latin )
Molecular formula C 33 H 50 N 4 O 6 S
External identifiers / databases
CAS number 126222-34-2
PubChem 6324659
DrugBank DB00212
Wikidata Q417432
Drug information
ATC code

C09 XA01

Drug class

Antihypertensive drugs

Mechanism of action

Inhibition of the protease renin

properties
Molar mass 630.84 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Remikiren is an experimental drug from the group of renin inhibitors for the treatment of high blood pressure .

Clinical information

Remikiren is still in clinical trials. The substance is a very effective renin inhibitor both in vitro , where it shows an IC 50 of 0.7 nmol·L −1 for human renin, and in vivo . In a short-term study of 8 days on the treatment of hypertension with 600 mg pure Remikiren as well as in combination with the diuretic hydrochlorothiazide , the pure substance proved to be ineffective, the combination with the diuretic, however, was significantly effective, without any side effects or intolerance.

literature

  • Pieter van Paassen, Dick de Zeeuw, Paul E. de Jong, Gerjan Navis: Renin Inhibition Improves Pressure Natriuresis in Essential Hypertension . In: Journal of the American Society of Nephrology . tape 11 , no. 10 , 2000, pp. 1813-1818 , PMID 11004211 (free full text).
  • Pieter van Paassen, Dick de Zeeuw, Gerjan Navis, Paul E. de Jong: Renal and systemic effects of continued treatment with renin inhibitor remikiren in hypertensive patients with normal and impaired renal function . In: Nephrology Dialysis Transplantation . tape 15 , no. 5 , 2000, pp. 637–643 , doi : 10.1093 / ndt / 15.5.637 (free full text).
  • Jasper J. Saris, Frans HM Derkx, René JA De Bruin, Dick HW Dekkers, Jos MJ Lamers, Pramod R. Saxena, Maarten ADH Schalkamp, ​​AH Jan Danser: High-affinity prorenin binding to cardiac man-6-P / IGF- II receptors precedes proteolytic activation to renin . In: American Journal of Physiology . Heart and Circulatory Physiology . tape 280 , no. 4 , 2001, p. H1706-1715 , PMID 11247783 (free full text).

Individual evidence

  1. This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  2. Luisa Quadri, Mauro Gobbini, Lamberto Monti: Recent Advances in Antihypertensive Therapy . In: Current Pharmaceutical Design . tape 4 , no. 6 , 1998, pp. 489-512 , PMID 10197059 ( limited preview in Google Book search).