title: Modulation of allergic and nonallergic histamine secretion by lipoxygenase inhibitors.
abstract: The ability of selected lipoxygenase inhibitors (LI) to influence allergic and nonallergic histamine secretion was studied. LI were found to exert concentration-dependent inhibition of allergic histamine release from rat peritoneal mast cells (RPMC) with the following IC50s, microM: nordihydroguaiaretic acid (NDGA) = 3.9; 5, 8, 11, 14-eicosatetraynoic acid (ETYA) = 3.8 and BW 755c = greater than 10. Calcium ionophore A23187 (0.2 microM)-induced histamine release from RPMC was also inhibited by these agents in a concentration-dependent fashion. The IC50s, microM were as follows: NDGA = 1.9; ETYA = 5.9 and BW 755c = greater than 10. Allergic histamine release from rabbit mixed leukocytes was inhibited by these drugs. The IC50s, microM, were as follows: NDGA = 1.4; BW 755c = 1.9 and ETYA = 7.2. These data suggest that the products of 5-lipoxygenase(s), e.g., 5-HPETE, 5-HETE, etc., may modulate (regulate) histamine secretion process(es).
mesh_terms: D015772:4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine; D015117:5,8,11,14-Eicosatetraynoic Acid / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D000001:Calcimycin / Q000494:pharmacology*; D002396:Catechols / Q000494:pharmacology*; D005231:Fatty Acids, Unsaturated / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects*; D006967:Hypersensitivity; D007700:Kinetics; D016859:Lipoxygenase Inhibitors; D009637:Masoprocol / Q000494:pharmacology*; D008407:Mast Cells / Q000187:drug effects / Q000276:immunology / Q000502:physiology*; D011720:Pyrazoles / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002396:Catechols; D005231:Fatty Acids, Unsaturated; D016859:Lipoxygenase Inhibitors; D011720:Pyrazoles; D015117:5,8,11,14-Eicosatetraynoic Acid; D000001:Calcimycin; D015772:4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine; D009637:Masoprocol