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.1 It does not displace [3H]-LTB4 binding to BLT1 at concentrations >1 µM and activates BLT2 at significantly lower concentrations than LTB4 (EC50 = 170 nM).1 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
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. J Biol Chem280(26)24816-24823(2005).
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CCCCC(=O)N(Cc1ccc(cc1)c1ccccc1C(=O)O)c1ccccc1
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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. J Biol Chem280(26)24816-24823(2005).
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