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Chemical Compound Review

CHEMBL17815     7-chloro-2-[(4- methoxyphenyl)methyl]-3...

Synonyms: AG-D-12121, SureCN6009815, ACMC-20m5l1, CHEBI:120283, CTK4A1301, ...
 
 
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Disease relevance of L-656224

 

High impact information on L-656224

  • In contrast L-656,224, a direct 5-lipoxygenase inhibitor, had no effect on the translocation of the enzyme [2].
  • Pretreatment with the 5-lipoxygenase inhibitor L-656,224 (15 mg/kg, 3.5 h pre-p.o.) before Ag challenge resulted in a significant inhibition (greater than 90%, p less than 0.05) of biliary leukotriene levels in this model [3].
  • Inhibition of human leukocyte 5-lipoxygenase by a 4-hydroxybenzofuran, L-656,224. Evidence for enzyme reduction and inhibitor degradation [4].
 

Biological context of L-656224

 

Associations of L-656224 with other chemical compounds

  • Ethanol (1 mL, p.o.)-induced haemorrhagic lesions were significantly reduced by prior oral administration of the 5-LO inhibitor L-656224 (50 mg/kg), whereas lower doses of this drug were ineffective [6].
 

Gene context of L-656224

  • L-656,224 (7-chloro-2-[(4-methoxyphenyl)methyl]-3- methyl-5-propyl-4-benzofuranol): a novel, selective, orally active 5-lipoxygenase inhibitor [1].

References

  1. L-656,224 (7-chloro-2-[(4-methoxyphenyl)methyl]-3- methyl-5-propyl-4-benzofuranol): a novel, selective, orally active 5-lipoxygenase inhibitor. Belanger, P., Maycock, A., Guindon, Y., Bach, T., Dollob, A.L., Dufresne, C., Ford-Hutchinson, A.W., Gale, P.H., Hopple, S., Lau, C.K. Can. J. Physiol. Pharmacol. (1987) [Pubmed]
  2. MK886, a potent and specific leukotriene biosynthesis inhibitor blocks and reverses the membrane association of 5-lipoxygenase in ionophore-challenged leukocytes. Rouzer, C.A., Ford-Hutchinson, A.W., Morton, H.E., Gillard, J.W. J. Biol. Chem. (1990) [Pubmed]
  3. The in vivo production of peptide leukotrienes after pulmonary anaphylaxis in the rat. Foster, A., Letts, G., Charleson, S., Fitzsimmons, B., Blacklock, B., Rokach, J. J. Immunol. (1988) [Pubmed]
  4. Inhibition of human leukocyte 5-lipoxygenase by a 4-hydroxybenzofuran, L-656,224. Evidence for enzyme reduction and inhibitor degradation. Rouzer, C.A., Riendeau, D., Falgueyret, J.P., Lau, C.K., Gresser, M.J. Biochem. Pharmacol. (1991) [Pubmed]
  5. Synthesis and structure-activity relationships of a novel class of 5-lipoxygenase inhibitors. 2-(Phenylmethyl)-4-hydroxy-3,5-dialkylbenzofurans: the development of L-656,224. Lau, C.K., Bélanger, P.C., Scheigetz, J., Dufresne, C., Williams, H.W., Maycock, A.L., Guindon, Y., Bach, T., Dallob, A.L., Denis, D. J. Med. Chem. (1989) [Pubmed]
  6. Effect of lipoxygenase inhibitors and leukotriene antagonists on acute and chronic gastric haemorrhagic mucosal lesions in ulcer models in the rat. Gyömber, E., Vattay, P., Szabo, S., Rainsford, K.D. J. Gastroenterol. Hepatol. (1996) [Pubmed]
 
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