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Chemical Compound Review

CGS-8515     methyl 2-[(3,4-dioxonaphthalen-1...

Synonyms: ACMC-1C4N1, AG-J-90901, SureCN3273068, AC1L4TWI, AC1Q5ZBK, ...
 
 
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Disease relevance of CGS 8515

  • 5. We conclude that leukotrienes have a major role in guinea-pig cardiac anaphylaxis, and that CGS 8515 has a cardio-protective action [1].
  • BW755c, CGS-8515, and FPL-55712 all prevented an otherwise significant fall in VF threshold during coronary occlusion (p less than 0.01) independent of an effect on effective refractory period, heart rate, or blood pressure [2].
  • The cyclooxygenase inhibitor aspirin (50 mg kg-1) and the dual cyclooxygenase/lipoxygenase inhibitor BW 755C (0.25-10.0 mg kg-1) were found to produce a significant protection against the arrhythmias, whereas aspirin (100 mg kg-1) and CGS 8515 were found to be ineffective [3].
 

High impact information on CGS 8515

 

Biological context of CGS 8515

  • 1. CGS 8515 selectively inhibited 5-LO (IC50 = 0.1 microM) with negligible effect on CO, 12-LO, 15-LO and TxS at concentrations up to 100 microM [8].
 

Anatomical context of CGS 8515

  • 4. CGS 8515, at oral doses as low as 5 mg/kg, significantly suppressed exudate volume and leukocyte migration in the carrageenan-induced pleurisy and sponge models in the rat [8].
 

Gene context of CGS 8515

 

Analytical, diagnostic and therapeutic context of CGS 8515

References

  1. Inhibition of leukotriene release in anaphylactic guinea-pig hearts by a 5-lipoxygenase inhibitor, CGS 8515. Yaacob, H.B., Piper, P.J. Br. J. Pharmacol. (1988) [Pubmed]
  2. Modulation of arachidonic acid metabolites and vulnerability to ventricular fibrillation during myocardial ischemia in the cat. Cooper, D.R., Kelliher, G.J., Kowey, P.R. Am. Heart J. (1988) [Pubmed]
  3. Effects of cyclooxygenase and lipoxygenase inhibitors on digoxin-induced arrhythmias and haemodynamics in guinea-pigs. Kanzik, I., Cakici, I., Ersoy, S., Ark, M., Abacioglu, N., Zengil, H. Pharmacol. Res. (1992) [Pubmed]
  4. Pharmacokinetic screening of o-naphthoquinone 5-lipoxygenase inhibitors. Rakhit, A., Kuwahara, S.K., Jones, D.R., Soliman, V.F., Kotake, A.N., Oglesby, T.D., Wasley, J.W., Tripp, S.L., Douglas, F.L. Pharm. Res. (1990) [Pubmed]
  5. Effect of 5-lipoxygenase and cyclooxygenase blockade on porcine hemodynamics during continuous infusion of platelet-activating factor. Olson, N.C., Kruse-Elliott, K.T., Johnson, L.W. Prostaglandins Leukot. Essent. Fatty Acids (1993) [Pubmed]
  6. Bradykinin-induced responses in a coaxial bioassay system composed of rat anococcygeus muscle and guinea pig trachea. Tunçtan, B., Cakici, I., Abacioğlu, N., Kanzik, I. Gen. Pharmacol. (1998) [Pubmed]
  7. Effects of platelet-activating factor antagonists WEB 2086 and BN 50730 on digoxin-induced arrhythmias. Cakici, I., Mataraci, N., Ersoy, S., Tunçtan, B., Abacioğlu, N., Kanzik, I. Pharmacol. Toxicol. (1995) [Pubmed]
  8. Characterization of CGS 8515 as a selective 5-lipoxygenase (5-LO) inhibitor. Ku, E.C., Raychaudhuri, A., Ghai, G., Kimble, E.F., Lee, W.H., Colombo, C., Dotson, R., White, D., Oglesby, T.D., Wasley, J.W. Adv. Prostaglandin Thromboxane Leukot. Res. (1989) [Pubmed]
  9. Characterization of CGS 8515 as a selective 5-lipoxygenase inhibitor using in vitro and in vivo models. Ku, E.C., Raychaudhuri, A., Ghai, G., Kimble, E.F., Lee, W.H., Colombo, C., Dotson, R., Oglesby, T.D., Wasley, J.W. Biochim. Biophys. Acta (1988) [Pubmed]
  10. CGS 8515 and indomethacin attenuate cytokine-induced cardiopulmonary dysfunction in pigs. Kruse-Elliott, K.T., Olson, N.C. Am. J. Physiol. (1993) [Pubmed]
  11. Determination of the 5-lipoxygenase inhibitor (CGS 8515) in plasma by high-performance liquid chromatography using reductive electrochemical detection. Kuwahara, S.K., Brubaker, W.F., Williams, E., Tripp, S., Douglas, F.L., Kotake, A.N. J. Chromatogr. (1990) [Pubmed]
 
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