ltb4 receptor การใช้

• To date, however, neither LTB4 synthesis inhibitors ( i . e . blockers of ALOX5 or LTA4 hydrolase ) nor inhibitors of LTB4 receptors ( BLT1 and BLT2 ) have turned out to be effective anti-inflammatory drugs.
• Several years after their identification of a Leukotriene B4 ( LTB4 ) receptor termed BLT1 or BLTR1 and encoded by the LTB4R1 gene, Shimizu and colleagues identified a second LTB4 receptor, BLT2 or BLTR2, encoded by the LTB4R2 gene.
• This byproduct differs from 5-oxo-ETE not only in the position and geometry of its double bounds but also in its activity : it stimulates human neutrophils apparently by acting on one or more LTB4 receptors rather than OXER1.
• Discovered several years after the leukotriene B4 receptor 1 ( BLT1 ), BLT2 receptor binds leukotriene B4 ( LTB4 ) with far lower affinity than the BLT1 receptor does and therefore has been termed the "'low affinity LTB4 receptor " '.
• The two BLT4-like receptors in Zebrafish, Blt2a and Blt2b, when transfected into chinese hamster ovary cells, mediate rises in cytosolic calcium responses to both 12-HHT and LTB4 with 12-HHT being about 500-to 1000-fold stronger that LTB4 in doing so; 12-HHT is inactive in this assay in chinese hamster ovary cells made to express the Zebrafish LTB4 receptor-1 ( Blt1 ).
• Based on the effects of LTB4 receptor antagonists, for example, leukotriene B4 receptor 2 mediates : the rise in cytosolic Ca2 + concentration ( a key signal for cell activation ) in human neutrophils and the rise in cytosolic Ca2 + concentration and chemotaxis in Chinese hamstery ovarian cells stimlated by 12 ( " S " )-HETE, 12 ( " R " )-HETE, and / or 12-oxo-ETE; the itch response to 12 ( " S " )-HETE triggered by the injection these metabolites into the skin of mice and guinea pigs, respectively; and an in vitro angiogenic response by Human umbilical vein endothelial cells ( HUVEC ) and in vivo angiogenic response by mice to 12 ( " S " )-HETE . The BLT2 receptor, in contrast to the GPR31 receptor, appears to be expressed at a high level in a wide range of tissues including neutrophils, eosinophils, monocytes, spleen, liver, and ovary.