Rostafuroxin

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Structural formula
Structural formula of rostafuroxin
General
Non-proprietary name Rostafuroxin
other names

21,23-epoxy-24-nor-14 β , 5 β -chola-20,21-diene-3 β , 14,17 α -triol

Molecular formula C 23 H 34 O 4
External identifiers / databases
CAS number 156722-18-8
PubChem 153976
ChemSpider 135709
DrugBank DB12350
Wikidata Q1110424
properties
Molar mass 374.52 g mol −1
safety instructions
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 .

Rostafuroxin (PST 2238) is a digitoxigenin - derivative serving as an antagonist of ouabain ( ouabain competitive) it from the Na + / K + -ATPase displaced.

The use of rostafuroxin was expected to be positive in chronic arterial hypertension , but in 2011 5 double-blind, crossover phase II studies in 410 hypertensive patients with (140-169 mm Hg) did not show any antihypertensive effects at any of the doses tested.

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. Staessen, YES. and Bianchi, G. (2005): Adducin and hypertension . In: Pharmacogenomics 6 (7); 665-9; PMID 16207143 ; PDF (free full text access).
  3. Manunta, P. (2001): A new antihypertensive agent that antagonizes the prohypertensive effect of endogenous ouabain and adducin. In: Cardiovasc. Hematol. Agents. Med. Chem. Vol. 4, pp. 61-66, PMID 16529550 .
  4. JA Staessen, L. Thijs u. a .: Main results of the ouabain and adducin for Specific Intervention on Sodium in Hypertension Trial (OASIS-HT): a randomized placebo-controlled phase-2 dose-finding study of rostafuroxin. In: Trials. Volume 12, January 2011, p. 13, doi : 10.1186 / 1745-6215-12-13 , PMID 21235787 , PMC 3031200 (free full text).

Web links

  • Ferrari, P. et al. (1998): PST2238: a new antihypertensive compound that antagonizes the long-term pressor effect of ouabain . In: J Pharmacol Exp Ther. 285 (1); 83-94; PMID 9535997 ; PDF (free full text access)
  • Iwamoto, T. and Kita, S. et al. (2006): Hypertension, Na + / Ca2 + exchanger, and Na +, K + -ATPase . In: Kidney Int . 69 (12); 2148-54; PMID 16641927