Leukotriene B4 (LTB4) promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, superoxide anion production, chemotaxis, and chemokinesis. Two G protein-coupled receptors, BLT1 and BLT2 mediate the actions of LTB4. CAY10583 is a potent, selective full agonist for BLT2 with an EC50 value of 20 nM. It does not displace [3H]-leukotriene B4 (LTB4) binding to BLT1 at concentrations >1 &#181M and activates BLT2 at significantly lower concentrations than LTB4 (EC50 = 170 nM). CAY10583 dose dependently increases intracellular calcium stores and induces ERK phosphorylation in Chinese hamster ovary (CHO) cells expressing BLT2 with no effect on CHO cells expressing BLT1.[1]

Reference:

[1]. Iizuka, Y., Yokomizo, T., Terawaki, K., et al. Characterization of a mouse second leukotriene B4 receptor, mBLT2. BLT2-dependent ERK activation and cell migration of primary mouse keratinocytes. The Journal of Biological Chemisty 280(26), 24816-24823 (2005

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