4'-[[(1-oxopentyl)phenylamino]methyl]-[1,1'-biphenyl]-2-carboxylic acid is a selective, potent full agonist for BLT2 (EC|50|= 20 nM). It does not displace [3H]-LTB4 binding to BLT1 at concentrations >1 μM and activates BLT2 at significantly lower concentrations than LTB|4|(EC|50|= 170 nM). 4'-[[(1-oxopentyl)phenylamino]methyl]-[1,1'-biphenyl]-2-carboxylic acid increases intracellular calcium stores in a dose-dependent manner, and induces ERK phosphorylation in Chinese hamster ovary (CHO) cells expressing BLT2 with no effect on CHO cells expressing BLT1.
1.Iizuka Y, Yokomizo T, Terawaki K, Komine M, Tamaki K, Shimizu T. (2005) Characterization of a mouse second leukotriene B4 receptor, mBLT2: BLT2-dependent ERK activation and cell migration of primary mouse keratinocytes.. J Biol Chem, 280 (26):(24816-23). [PMID:15866883][10.1021/op500134e]
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