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Chemical Compound Review

Octimibate     8-(1,4,5-triphenylimidazol- 2...

Synonyms: Octimibato, Octimibatum, CHEMBL419952, SureCN382403, AC1L23QE, ...
 
 
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High impact information on Octimibate

  • Therefore, the poor coupling of the IP receptor in SK-N-SH cells to G(q) is unlikely to explain the relatively low efficacy of octimibate for stimulating adenylyl cyclase in these cells [1].
  • Since octimibate shows extensive species variation and is potent at inhibiting platelet aggregation in primates, all of the experiments reported here have been carried out with primate tissue or in vivo in cynomolgus monkeys [2].
  • In platelet-rich plasma, octimibate inhibits agonist-stimulated aggregation with an IC50 of approx. 200 nM [3].
  • Octimibate stimulates adenylyl cyclase activity in human platelet membranes, with an EC50 of 200 nM [3].
  • Octimibate, a potent non-prostanoid inhibitor of platelet aggregation, acts via the prostacyclin receptor [3].
 

Biological context of Octimibate

 

Anatomical context of Octimibate

 

Associations of Octimibate with other chemical compounds

 

Gene context of Octimibate

References

  1. Factors affecting prostacyclin receptor agonist efficacy in different cell types. Kam, Y., Chow, K.B., Wise, H. Cell. Signal. (2001) [Pubmed]
  2. Primate vascular responses to octimibate, a non-prostanoid agonist at the prostacyclin receptor. Merritt, J.E., Brown, A.M., Bund, S., Cooper, D.G., Egan, J.W., Hallam, T.J., Heagerty, A.M., Hickey, D.M., Kaumann, A.J., Keen, M. Br. J. Pharmacol. (1991) [Pubmed]
  3. Octimibate, a potent non-prostanoid inhibitor of platelet aggregation, acts via the prostacyclin receptor. Merritt, J.E., Hallam, T.J., Brown, A.M., Boyfield, I., Cooper, D.G., Hickey, D.M., Jaxa-Chamiec, A.A., Kaumann, A.J., Keen, M., Kelly, E. Br. J. Pharmacol. (1991) [Pubmed]
  4. Octimibate inhibition of platelet aggregation: stimulation of adenylate cyclase through prostacyclin receptor activation. Seiler, S., Brassard, C.L., Arnold, A.J., Meanwell, N.A., Fleming, J.S., Keely, S.L. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  5. Prostacyclin agonists reduce early atherosclerosis in hyperlipidemic hamsters. Octimibate and BMY 42393 suppress monocyte chemotaxis, macrophage cholesteryl ester accumulation, scavenger receptor activity, and tumor necrosis factor production. Kowala, M.C., Mazzucco, C.E., Hartl, K.S., Seiler, S.M., Warr, G.A., Abid, S., Grove, R.I. Arterioscler. Thromb. (1993) [Pubmed]
  6. The inhibitory effects of non-prostanoid prostacyclin mimetics on rat neutrophil function. Wise, H. Prostaglandins Leukot. Essent. Fatty Acids (1996) [Pubmed]
  7. Effects of octimibate, an inhibitor of acyl coenzyme A: cholesterol acyltransferase, on cholesterol metabolism in the hamster and rat. Jackson, B., Gee, A., Black, S., Suckling, K.E. Biochem. Pharmacol. (1990) [Pubmed]
 
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