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Chemical Compound Review

Isbogrel     (E)-7-phenyl-7-pyridin-3-yl- hept-6-enoic acid

Synonyms: Isbogrelum, SureCN4060, Isbogrel [INN], CHEMBL26820, CCRIS 7236, ...
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Disease relevance of Isbogrel


High impact information on Isbogrel


Chemical compound and disease context of Isbogrel


Biological context of Isbogrel

  • CV-4151 was equipotent to OKY-1580 (IC50: 2.3 X 10 M), a well documented TXA2 synthetase inhibitor, in an in vitro TXA2 synthetase assay [8].

Anatomical context of Isbogrel


Associations of Isbogrel with other chemical compounds


Analytical, diagnostic and therapeutic context of Isbogrel

  • Increase in TXB2 release into the great coronary vein during reperfusion was completely inhibited by CV-4151, whereas release of 6-keto-PGF1 alpha tended to increase during occlusion and reperfusion [5].
  • In rats, serial oral administration of CV-4151 (10 mg/kg) once daily for 14 days produced a constant and marked reduction of serum TXB2 concentration with concomitant increase of serum immunoreactive 6-keto-PGF1 alpha concentration [8].
  • In contrast, premedication with CV-4151 significantly improved the recovery of ATP (p < 0.01) [10].
  • The sham group (n = 8) underwent the operation without ischemia-reperfusion; the control group (n = 8) with ischemia-reperfusion, and the CV-4151 group (n = 8) was pretreated with CV-4151 20 mg/kg [10].
  • PCR showed the same tendency as ATP; CV-4151 also improved the recovery of PCR significantly (p < 0.05), but CV-4151 did not prevent the production of lipid peroxides [10].


  1. Involvement of thromboxane A2, leukotrienes and free radicals in puromycin nephrosis in rats. Shibouta, Y., Terashita, Z., Imura, Y., Shino, A., Kawamura, M., Ohtsuki, K., Ohkawa, S., Nishikawa, K., Fujiwara, Y. Kidney Int. (1991) [Pubmed]
  2. The thromboxane A2/prostaglandin endoperoxide receptor antagonist activity of CV-4151, a thromboxane A2 synthetase inhibitor. Imura, Y., Terashita, Z., Shibouta, Y., Nishikawa, K. Eur. J. Pharmacol. (1988) [Pubmed]
  3. Delay of the initiation of hypertension in spontaneously hypertensive rats by CV-4151, a specific thromboxane A2 synthetase inhibitor. Shibouta, Y., Terashita, Z., Inada, Y., Nishikawa, K. Eur. J. Pharmacol. (1985) [Pubmed]
  4. Beneficial effect of CV-4151 (Isbogrel), a thromboxane A2 synthase inhibitor, in a rat middle cerebral artery thrombosis model. Imura, Y., Kiyota, Y., Nagai, Y., Nishikawa, K., Terashita, Z. Thromb. Res. (1995) [Pubmed]
  5. Protective effect of a novel thromboxane synthetase inhibitor, CV-4151, on myocardial damage due to coronary occlusion and reperfusion in the hearts of anesthetized dogs. Imamoto, T., Terashita, Z., Tanabe, M., Nishikawa, K., Hirata, M. J. Cardiovasc. Pharmacol. (1986) [Pubmed]
  6. Comparison of GR32191, R68070 and CV-4151 upon U-46619- and collagen-induced platelet aggregation in vitro and ex vivo. Watts, I.S., White, B.P., Wharton, K.A., Lumley, P. Br. J. Pharmacol. (1989) [Pubmed]
  7. Effects of thromboxane A2 synthase inhibitors (CV-4151 and ozagrel), aspirin, and ticlopidine on the thrombosis caused by endothelial cell injury. Terashita, Z., Imura, Y., Kawamura, M., Kato, K., Nishikawa, K. Thromb. Res. (1995) [Pubmed]
  8. CV-4151--a potent, selective thromboxane A2 synthetase inhibitor. Terashita, Z., Imura, Y., Tanabe, M., Kawazoe, K., Nishikawa, K., Kato, K., Terao, S. Thromb. Res. (1986) [Pubmed]
  9. The role of thromboxane (TX) A2 in rabbit arterial thrombosis induced by endothelial damage. Imura, Y., Terashita, Z., Nishikawa, K. Thromb. Res. (1990) [Pubmed]
  10. Effects of thromboxane A2 synthetase inhibitor (CV-4151) on reperfused skeletal muscle in rats. Sasaki, Y., Ishiguro, N., Miura, T. European surgical research. Europäische chirurgische Forschung. Recherches chirurgicales européennes. (1994) [Pubmed]
  11. Randomized trial of a selective inhibitor of thromboxane A2 synthetase, (E)-7-phenyl-7-(3-pyridyl)-6-heptenoic acid (CV-4151), for prevention of restenosis after coronary angioplasty. Hattori, R., Kodama, K., Takatsu, F., Yui, Y., Kawai, C. Jpn. Circ. J. (1991) [Pubmed]
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