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Chemical Compound Review

Taprostene     3-[(Z)-[(1R,5S,7R,8S)-8- [(E,3S)-3...

Synonyms: Taprosteno, Taprostenum, AC1NSKAK, SureCN364129, CHEMBL2104890, ...
 
 
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Disease relevance of Taprostene

  • The effects of taprostene, a synthetic prostacyclin analogue, were investigated in a 6-hour model of myocardial ischemia (MI) with reperfusion in anesthetized cats [1].
  • Thus, taprostene exerted a significant cardioprotection in cats subjected to ischemia and reperfusion.(ABSTRACT TRUNCATED AT 250 WORDS)[1]
  • In a placebo-controlled dose rising study, taprostene or placebo was intravenously infused in 80 patients treated with the thrombolytic agent saruplase (rscu-PA) for acute myocardial infarction [2].
  • It is assumed that taprostene may be of clinical benefit in patients with ischaemic peripheral vascular disease [3].
  • Taprostene, infused in a dose (0.1 microgram/kg.min, i.v.) that inhibited ADP-induced decrease of circulating platelets by 56%, reduced the total thrombus weight (p less than 0.05 vs control) and in combination it further augmented the saruplase (21.5 micrograms/kg.min)-induced thrombolysis (p less than 0.05 vs saruplase alone) [4].
 

High impact information on Taprostene

 

Biological context of Taprostene

 

Anatomical context of Taprostene

 

Associations of Taprostene with other chemical compounds

  • Similarly, on rat tail artery contracted with phenylephrine, 3 microM taprostene (20% relaxation) opposed AFP-07- but not PGE2-induced relaxation [9].
  • In order to assess the effect of taprostene on haemodynamics, platelet function and arachidonate metabolism in 4 healthy volunteers an intravenous infusion of 25 ng.kg-1.min-1 was given for 6 h [14].
  • Antiaggregatory action of taprostene was demonstrated towards arachidonic acid-, ADP-, thrombin- and norepinephrine-induced aggregations of human platelet rich plasma with IC50 values between 17 and 34 nmol/l. ADP-induced aggregations of human, dog or rabbit platelets were inhibited with an equivalent efficacy [15].
  • Pilot study of the effects of taprostene (CG 4203) in patients with advanced peripheral arterial disease [16].
 

Gene context of Taprostene

 

Analytical, diagnostic and therapeutic context of Taprostene

  • Taprostene (100 ng/kg/min) was infused intravenously starting 30 minutes postocclusion of the left anterior descending coronary artery followed by reperfusion 1 hour later, and the cats were observed for an additional 4.5 hours [1].
  • Although taprostene did not affect 90 min patency, there was a trend to better maintenance of patency after rescue PTCA [2].
  • Intra-arterial infusion of taprostene into the rabbit inhibited ADP-induced aggregation ex vivo with an ED50 value of 0.49 micrograms/kg/min [8].

References

  1. Endothelium and myocardial protecting actions of taprostene, a stable prostacyclin analogue, after acute myocardial ischemia and reperfusion in cats. Johnson, G., Furlan, L.E., Aoki, N., Lefer, A.M. Circ. Res. (1990) [Pubmed]
  2. The effect of taprostene in patients with acute myocardial infarction treated with thrombolytic therapy: results of the START study. Saruplase Taprostene Acute Reocclusion Trial. Bär, F.W., Meyer, J., Michels, R., Uebis, R., Lange, S., Barth, H., Groves, R., Vermeer, F. Eur. Heart J. (1993) [Pubmed]
  3. Effects of taprostene, a chemically stable prostacyclin analogue, in patients with ischaemic peripheral vascular disease: a placebo controlled double-blind trial. Virgolini, I., Fitscha, P., O'Grady, J., Barth, H., Sinzinger, H. Prostaglandins Leukot. Essent. Fatty Acids (1989) [Pubmed]
  4. Taprostene, a stable prostacyclin analogue, enhances the thrombolytic efficacy of saruplase (recombinant single-chain urokinase-type plasminogen activator) in rabbits with pulmonary embolized thrombi. Schneider, J. Prostaglandins (1991) [Pubmed]
  5. Vascular endothelial growth factor/vascular permeability factor enhances vascular permeability via nitric oxide and prostacyclin. Murohara, T., Horowitz, J.R., Silver, M., Tsurumi, Y., Chen, D., Sullivan, A., Isner, J.M. Circulation (1998) [Pubmed]
  6. The mechanisms of enhancement and inhibition of field stimulation responses of guinea-pig vas deferens by prostacyclin analogues. Tam, F.S., Chan, K., Borreau, J.P., Jones, R.L. Br. J. Pharmacol. (1997) [Pubmed]
  7. Beneficial effects of the prostacyclin analogue taprostene on cardiovascular, pulmonary and renal disturbances in endotoxin-shocked rabbits. Schneider, J. Eicosanoids (1991) [Pubmed]
  8. In vivo studies with the stabilized epoprostenol analogue taprostene. Effects on platelet functions and blood clotting. Michel, G., Seipp, U. Arzneimittel-Forschung. (1990) [Pubmed]
  9. Partial agonism of taprostene at prostanoid IP receptors in vascular preparations from guinea-pig, rat, and mouse. Chan, K.M., Jones, R.L. J. Cardiovasc. Pharmacol. (2004) [Pubmed]
  10. Effects of taprostene on neutrophil-endothelial interactions in isolated coronary arteries. Lefer, A.M., Murohara, T., Buerke, M. Methods and findings in experimental and clinical pharmacology. (1994) [Pubmed]
  11. Neutrophil count and amputation in critical limb ischaemia. Belch, J.J., Söhngen, M., Robb, R., Voleske, P., Söhngen, W. International angiology : a journal of the International Union of Angiology. (1999) [Pubmed]
  12. Effects of prostacyclin and taprostene in splanchnic artery occlusion shock. VanAntwerp, D.R., Hedley, L.R., Spires, D.A., Strosberg, A.M., Johnson, G., Lefer, A.M. Eicosanoids (1991) [Pubmed]
  13. Effects of prostacyclin on hearing recovery after repetitive noise and on histomorphology of the inner ear in the guinea pig. Michel, O., Walger, M., Schrott-Fischer, A. ORL J. Otorhinolaryngol. Relat. Spec. (1994) [Pubmed]
  14. Effects of taprostene, a stable prostacyclin analogue, on haemodynamics, platelet function and arachidonate metabolism in healthy volunteers. Virgolini, I., Fitscha, P., Sinzinger, H., Barth, H. Eur. J. Clin. Pharmacol. (1990) [Pubmed]
  15. In vitro studies with the stabilized epoprostenol analogue taprostene. Effect on platelets and erythrocytes. Michel, G., Seipp, U. Arzneimittel-Forschung. (1990) [Pubmed]
  16. Pilot study of the effects of taprostene (CG 4203) in patients with advanced peripheral arterial disease. Darius, H., Kopp, H., Mulfinger, A., Spielberger, M., Todt, M., Schuster, C.J., Meyer, J. Prog. Clin. Biol. Res. (1989) [Pubmed]
  17. Agonists can discriminate between cloned human and mouse prostacyclin receptors. Chow, K.B., Jones, R.L., Wise, H. Prostaglandins Leukot. Essent. Fatty Acids (2004) [Pubmed]
  18. In vitro analysis of synergistic effects of fibrinolytic agents and prostacyclin analogues. Spiecker, M., Heinke, B., Meyer, J., Darius, H. Haemostasis (1997) [Pubmed]
  19. Additional myocardial salvage by coadministration of the epoprostenol analog taprostene to recombinant single-chain urokinase-type plasminogen activator in a canine coronary thrombosis model. Groves, R., Schneider, J., Friderichs, E., Giertz, H., Flohé, L. Arzneimittel-Forschung. (1989) [Pubmed]
 
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