Leukotriene B4 (LTB4) is a potent chemotactic agent and activating factor for granulocytes. Two cell surface receptors for LTB4 (BLT1 and BLT2) have been isolated in the last few years. These receptors are G-protein-coupled receptors (GPCR), and they have 45% amino acid identity. BLT1 and BLT2 are high- and low- affinity receptors, respectively. Cells transfected with BLT1 and BLT2 show LTB4-dependent intracellular signal transduction and chemotaxis in vitro. The distribution and pharmacological characteristics of BLT1 and BLT2 are different, suggesting distinct roles for these receptors in vivo. The open reading frame (ORF) of BLT2 overlaps the promoter of BLT1, a so called 'promoter in ORF'. Based on recent publications on BLT1 transgenic and knock out mice phenotypes, it appears that LTB4 plays important roles in inflammation in addition to host defense in vivo.