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Uptodate Reference Title
Leukotriene modifiers
Leukotriene modifiers
Source cells include mast cells, eosinophils, basophils, and macrophages. Zileuton inhibits 5-lipoxygenase (5-LO), while montelukast, zafirlukast, and pranlukast are antagonists of the CysLT1 receptor.
PLA2: phospholipase A2; AA: arachidonic acid; 5-LO: 5-lipoxygenase; FLAP: 5-LO activating protein; LTA4: leukotriene A4; LTA4H: LTA4 hydrolase; LTC4S: LTC4 synthetase; LTB4: leukotriene B4 arises from the hydrolysis of LTA4 by LTA4 hydrolase; LTC4: leukotriene C4 arises from the conjugation of LTA4 with reduced glutathione by LTC4 synthetase; LTD4: leukotriene D4 arises from LTC4 by the rapid removal of glutamic acid in the extracellular microenvironment; LTE4: leukotriene E4 arises from LTD4 by the further removal of glycine in the extracellular microenvironment; BLT1: receptor for LTB4, no commercially available inhibitors; BLT2: receptor for LTB4, no commercially available inhibitors; CysLTS: cys-leukotrienes, LTC4, LTD4, LTE4; CysLT1: receptor for LTC4, LTD4, LTE4, inhibited by montelukast, pranlukast, and zafirlukast; CysLT2: receptor for LTC4, LTD4, LTE4, but not inhibited by montelukast, pranlukast, or zafirlukast.
