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

Abstract
L-656,224 (7-chloro-2-[(4-methoxyphenyl)methyl]-3-methyl-5-propyl-4-benzofuranol) was a potent inhibitor of leukotriene biosynthesis in intact rat and human leukocytes and CXBG mastocytoma cells (IC50 values, 18-240 nM) and of crude human leukocyte and highly purified porcine leukocyte 5-lipoxygenase (IC50 value, 4 X 10(-7) M). The selectivity of L-656,224 for 5-lipoxygenase was shown through the relative lack of activity of the compound on 12-lipoxygenase, 15-lipoxygenase, cyclooxygenase, catalase, and myeloperoxidase. The compound showed (i) oral activity against hyperalgesia induced in the rat paw by injection of yeast or platelet-activating factor, (ii) dyspnea in sensitized inbred rats induced by an aerosol of antigen, and (iii) bronchoconstriction induced by an aerosol of Ascaris in squirrel monkeys, suggesting a role for 5-lipoxygenase inhibitors in the treatment of asthma and peripheral pain.
AuthorsP Belanger, A Maycock, Y Guindon, T Bach, A L Dollob, C Dufresne, A W Ford-Hutchinson, P H Gale, S Hopple, C K Lau
JournalCanadian journal of physiology and pharmacology (Can J Physiol Pharmacol) Vol. 65 Issue 12 Pg. 2441-8 (Dec 1987) ISSN: 0008-4212 [Print] Canada
PMID2835137 (Publication Type: Journal Article)
Chemical References
  • Benzofurans
  • Lipoxygenase Inhibitors
  • L 656224
  • Catalase
  • Peroxidase
  • Arachidonate Lipoxygenases
  • Prostaglandin-Endoperoxide Synthases
Topics
  • Animals
  • Arachidonate Lipoxygenases (antagonists & inhibitors)
  • Benzofurans (pharmacology)
  • Blood Platelets (enzymology)
  • Catalase (antagonists & inhibitors)
  • Cattle
  • Cells, Cultured
  • Eating (drug effects)
  • Female
  • Humans
  • Leukocytes (enzymology)
  • Lipoxygenase Inhibitors
  • Neutrophils (enzymology)
  • Peroxidase (metabolism)
  • Prostaglandin-Endoperoxide Synthases (metabolism)
  • Rats
  • Saimiri
  • Soybeans (enzymology)
  • Species Specificity
  • Swine

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