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Chemical Compound Review

AGN-PC-00YM1E     4-[3-[5-[5-(4,5-dihydroxy-6- methyl-oxan-2...

Synonyms: NSC-95099, NSC95099, AR-1F1318, AC1L66EK, MLS002701944, ...
 
 
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Disease relevance of Gitoxim

 

High impact information on Gitoxim

  • After in vitro perfusion of rabbit isolated liver with an emulsion of perfluorocarbon containing [3H]gitoxin, the radioactivity in the liver and in the bile was the sum of that contained in a volatile fraction (tritiated water due to metabolism of gitoxin) and that contained in a nonvolatile fraction (gitoxin and its metabolites) [3].
  • The method detection limits were 0.05 microg/g for oleandrin, 0.1 microg/g for gitoxin, and 0.2 microg/g for the other toxicants in gastrointestinal contents and feces and were 5 times higher in plant material [4].
  • A two-dimensional thin-layer chromatographic method was developed for the qualitative determination of the cardiotoxins oleandrin, gitoxin, digitoxin, gitoxigenin, and grayanotoxins I, II, and III in gastrointestinal contents (stomach, rumen, colon, and cecum contents), feces, and plant material [4].
  • Compared to ouabain and gitoxin, it produces positive inotropic effects on the isolated guinea-pig heart in a wider range of concentrations and causes less pronounced rhythmic disturbances [5].
  • The results show that the zein microspheres obtained using ethanol are best suited for use as a sustained-release form of Gitoxin [6].
 

Biological context of Gitoxim

 

Anatomical context of Gitoxim

  • The data obtained in plasma and in myocardium between 1 and 6 hr after administration of digoxin or gitoxin show that the distribution of the unchanged cardiac glycoside and each chloroform-soluble metabolite, from plasma to myocardium, is achieved 1 hr after administration [11].
  • When administered as hydroalcoholic solutions into the stomach or into the duodenum, gitoxin is nearly completely absorbed (94.5%) [12].
  • Inhibition of Na+/K+-ATPase activity from human erythrocyte membranes and commercial porcine cerebral cortex by in vitro single and simultaneous exposure to digoxin and gitoxin was investigated to elucidate the difference in the mechanism of the enzyme inhibition by structurally different cardiac glycosides [13].
 

Associations of Gitoxim with other chemical compounds

 

Analytical, diagnostic and therapeutic context of Gitoxim

References

  1. Complementary combining site contact residue mutations of the anti-digoxin Fab 26-10 permit high affinity wild-type binding. Short, M.K., Krykbaev, R.A., Jeffrey, P.D., Margolies, M.N. J. Biol. Chem. (2002) [Pubmed]
  2. Anti-tumour activity of Digitalis purpurea L. subsp. heywoodii. López-Lázaro, M., Palma De La Peña, N., Pastor, N., Martín-Cordero, C., Navarro, E., Cortés, F., Ayuso, M.J., Toro, M.V. Planta Med. (2003) [Pubmed]
  3. Hepatic clearance of gitoxin. Metabolism and biliary excretion by rabbit isolated liver. Pellegrin, P.L., Lesne, M. Drug Metab. Dispos. (1984) [Pubmed]
  4. Multiresidue screen for cardiotoxins by two-dimensional thin-layer chromatography. Holstege, D.M., Francis, T., Puschner, B., Booth, M.C., Galey, F.D. J. Agric. Food Chem. (2000) [Pubmed]
  5. Therapeutic range of cardiac glycosides. Haustein, K.O. Basic Res. Cardiol. (1984) [Pubmed]
  6. Simple coacervates of zein to encapsulate Gitoxin. Muthuselvi, L., Dhathathreyan, A. Colloids and surfaces. B, Biointerfaces. (2006) [Pubmed]
  7. A further study of the pharmacokinetics of gitoxin in rabbit isolated liver: clearance of 3H-gitoxin. Pellegrin, P.L., Lesne, M. European journal of drug metabolism and pharmacokinetics. (1985) [Pubmed]
  8. Bioavailability study of gitoxin in a solid dosage form. Hupin, C., de Suray, J.M., Versluys, J., Lorent, M., Dodion, L., Lesne, M. International journal of clinical pharmacology and biopharmacy. (1979) [Pubmed]
  9. Studies on the pharmacokinetics and the metabolism of gitoxin in the guinea-pig: I. Disposition kinetics following an i.v. bolus of 3H-gitoxin. Kadima, L.N., Lesne, M. Archives internationales de pharmacodynamie et de thérapie. (1980) [Pubmed]
  10. Hepatic clearance of gitoxin: pharmacokinetic study on rabbit isolated liver. Influence of protein binding and comparison with digoxin. Pellegrin, P., Lesne, M. European journal of drug metabolism and pharmacokinetics. (1983) [Pubmed]
  11. Cardiac glycosides and their metabolites levels in plasma and heart of guinea-pigs after I. V. administration. Dolphen, R., Lesne, M. Archives internationales de pharmacodynamie et de thérapie. (1981) [Pubmed]
  12. Studies on the pharmacokinetics and the metabolism of gitoxin in the guinea-pig: II. the enteral absorption and the enterohepatic recirculation. Kadima, L.N., Lesne, M. Archives internationales de pharmacodynamie et de thérapie. (1982) [Pubmed]
  13. Effects of digoxin and gitoxin on the enzymatic activity and kinetic parameters of Na+/K+-ATPase. Krstić, D., Krinulović, K., Spasojević-Tisma, V., Joksić, G., Momić, T., Vasić, V. Journal of enzyme inhibition and medicinal chemistry. (2004) [Pubmed]
  14. The binding of gitoxin to human plasma proteins. Verbeke, N., Pellegrin, P., Vienne, A., Lesne, M. Eur. J. Clin. Pharmacol. (1979) [Pubmed]
  15. Some pharmacological studies on the cardiotonic effects of furanosteroidal glycosides. Matsumura, S., Kimoto, S., Uno, O., Minesita, T., Ueda, M. Archives internationales de pharmacodynamie et de thérapie. (1977) [Pubmed]
  16. Uptake and pharmacological effect of gitoxin and gitaloxin in rat and guinea-pig perfused hearts. Comparison with digitoxin and digoxin. Dolphen, R., Lesne, M. Arzneimittel-Forschung. (1980) [Pubmed]
  17. Reverse phase thin layer chromatographic procedure for identification of digoxin and related fluorescing substances. Bloch, D.E. Journal - Association of Official Analytical Chemists. (1980) [Pubmed]
  18. Pharmacological reevaluation of gitoxin in man. Lesne, M. International journal of clinical pharmacology and biopharmacy. (1978) [Pubmed]
 
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