title: Inhibition of lipid mediator biosynthesis in human inflammatory cells by BIRM 270.
abstract: BIRM 270 was developed as a potent and enantioselective inhibitor of LTB4 biosynthesis by human neutrophils, and was also found to inhibit LTC4 production by human eosinophils and lung mast cells. BIRM 270 inhibited LTB4 synthesis in neutrophils by preventing arachidonate release from membrane phospholipids, and over the same concentration range, inhibited PAF biosynthesis. BIRM 270 did not directly inhibit acylhydrolases which have been implicated in eicosanoid and PAF biosynthesis, suggesting an indirect mode of action.
authors.affiliation: Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06877, USA.
authors.forename: T P
authors.initials: TP
authors.lastname: Parks
authors.forename: A F
authors.initials: AF
authors.lastname: Hoffman
authors.forename: C A
authors.initials: CA
authors.lastname: Homon
authors.forename: A G
authors.initials: AG
authors.lastname: Graham
authors.forename: E S
authors.initials: ES
authors.lastname: Lazer
authors.forename: F H
authors.initials: FH
authors.lastname: Chilton
authors.forename: P
authors.initials: P
authors.lastname: Borgeat
authors.forename: D
authors.initials: D
authors.lastname: Raible
authors.forename: E
authors.initials: E
authors.lastname: Schulman
authors.forename: D A
authors.initials: DA
authors.lastname: Bass
mesh_terms: D016718:Arachidonic Acid / Q000037:antagonists & inhibitors*; D001583:Benzoxazoles / Q000494:pharmacology*; D004804:Eosinophils / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D007249:Inflammation / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D015289:Leukotrienes / Q000096:biosynthesis*; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism
chemical_list: D001583:Benzoxazoles; D015289:Leukotrienes; D016718:Arachidonic Acid; C090950:ontazolast