5,8,11,14-Eicosatetraynoic acid (ETYA) inhibits binding of N-formyl-methionyl-leucyl-phenylalanine (FLMP) to its receptor on human granulocytes. A note of caution.
Binding of two biochemically chemotactic factors, FMLP and C5a, to their respective receptors on human granulocytes produces a transient several-fold increase in cAMP. To determine if arachidonic acid metabolites were responsible for the increased cAMP concentrations, two inhibitors of arachidonic acid metabolism, indomethacin and ETYA, were incubated with granulocytes prior to FMLP or C5A. ETYA, but not indomethacin, inhibited both the cAMP and superoxide responses to a similar degree. However, the mechanism of this effect was found to be through inhibition of the binding of FMLP to its receptor rather than through inhibition of arachidonate metabolism.
D015117:5,8,11,14-Eicosatetraynoic Acid / Q000494:pharmacology*; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000378:metabolism; D003182:Complement C5 / Q000378:metabolism; D015936:Complement C5a; D000242:Cyclic AMP / Q000378:metabolism; D005231:Fatty Acids, Unsaturated / Q000494:pharmacology*; D006098:Granulocytes / Q000378:metabolism*; D006801:Humans; D007213:Indomethacin / Q000494:pharmacology; D008715:Methionine / Q000031:analogs & derivatives*; D009239:N-Formylmethionine / Q000031:analogs & derivatives* / Q000378:metabolism; D009240:N-Formylmethionine Leucyl-Phenylalanine; D009842:Oligopeptides / Q000378:metabolism*; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D044042:Receptors, Formyl Peptide
D001095:Arachidonic Acids; D003182:Complement C5; D005231:Fatty Acids, Unsaturated; D009842:Oligopeptides; D011956:Receptors, Cell Surface; D044042:Receptors, Formyl Peptide; D015117:5,8,11,14-Eicosatetraynoic Acid; D016718:Arachidonic Acid; D009239:N-Formylmethionine; D009240:N-Formylmethionine Leucyl-Phenylalanine; D015936:Complement C5a; D008715:Methionine; D000242:Cyclic AMP; D007213:Indomethacin