blt2

LY255283 是白三烯 B4 (LTB4) 受体的特异性拮抗剂，抑制人外周血多形核白细胞和由钙离子载体 A23187 激活的单核细胞中 LTB(4) 的产生。

BLT2 agonist-1 (compound 15b) 是选择性BLT2拮抗剂，能在224 nM IC50下抑制CHO-BLT2细胞趋化性。它不影响CHO-BLT1细胞趋化性，并在132 nM Ki值下抑制LTB4与BLT2结合。BLT2 agonist-1适用于哮喘、慢性阻塞性肺病等炎症性气道疾病研究。

BLT2 probe 1 (化合物 13) 是一款以 CAY10583 合成激动剂为基础的荧光探针，主要靶向糖尿病伤口愈合和胃肠道病变中潜在的 BLT2。该探针适用于多种检测系统中对 BLT2 受体配体进行药理学研究。

Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from arachidonic acid through the 5-lipoxygenase pathway. It promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, enhancement of lysosomal enzyme release, superoxide anion production, chemotaxis, and chemokinesis. At least two LTB4 receptors, termed BLT1 and BLT2, have been identified. 14,15-dehydro LTB4 is a LTB4 receptor antagonist that has a higher binding affinity for BLT1, demonstrating a Ki value of 27 nM, compared to BLT2, which has a Ki value of 473 nM. 14,15-dehydro LTB4 inhibits LTB4-induced release of lysozymes from rat polymorphonuclear leukoctyes with an IC50 value of 1 μM.

Leukotriene B4 (LTB4)-3-aminopropylamide is an analog of LTB4 that exhibits potent and selective binding to the BLT1 receptor with Ki values of 5.1 nM at BLT1 and 1,227 nM at BLT2, indicating its high affinity for BLT1 over BLT2. This compound's effects are mediated through interactions with two receptors, BLT1 and BLT2.

The effects of Leukotriene B4 (LTB4) are mediated by two known receptors, BLT1 and BLT2. LTB4 is a high affinity ligand for BLT1, and many of its pro-inflammatory effects are believed to be transduced through this receptor. The BLT2 is more enigmatic, in that LTB4 is not a high-affinity ligand, nor is it clear that BLT2 activation promotes inflammation. LTB4 ethanolamide (LTB4-EA) is a theoretical 5-LO metabolite of arachidonoyl ethanolamide (AEA). In CHO cells transfected with human BLTR1, LTB4-EA was a potent antagonist with about three times greater affinity for the receptor than LTB4 (Ki = 1.22 nM versus 3.88 nM). LTB4-EA antagonizes the LTB4-induced contractions of guinea pig lung parenchyma with an EC50 of 10 nM. LTB4-EA thus represents a potential endogenous anti-inflammatory compound functioning as a natural antagonist of BLTR1.

CAY10583 is an agonist of leukotriene B4 receptor type 2 (BLT2). CAY10583 directly promotes keratinocyte migration and indirectly enhances fibroblast proliferation by increasing keratinocyte production of bFGF1 and TGF-β, leadng to accelerate wound closur

Leukotriene B4 (LTB4) compounds are produced by both enzymatic and non-enzymatic processes. The products of enzymatic origin, via Leukotriene A4 (LTA4) hydrolase, are stereospecifically 12(R). Non-enzymatic hydrolysis products are 50:50 mixtures at C-12, but are almost exclusively trans at C-6. Thus, the non-enzymatic hydrolysis product of LTA4 is 6-trans-12-epi LTB4. 12-epi LTB4 is an isomer which would not be expected to occur in either non-enzymatic hydrolysis products, or in the enzymatic products of LTA4 hydrolase. Compared to LTB4, 12-epi LTB4 has significantly reduced activity for the LTB4 receptor on human neutrophils (IC50 of 7.5 mM), and on guinea pig lung membranes with a (Ki of 4.7 mM). 12-epi LTB4 is an weak agonist at both the recombinant human BLT1 and BLT2 receptors, requiring approximately 10 mM for full activation of the receptor.

T-10430 是一种具有口服活性的有效白三烯 B4 受体 2 (leukotriene B4 receptor 2 (BLT2)) 激动剂，具有用于银屑病研究的潜力。

20-hydroxy LTB4 is a metabolite of LTB4 in human neutrophils. In human leukocytes, LTB4 is inactivated by the enzyme LTB4 20-hydroxylase. 20-hydroxy LTB4 is not only much less active (~5%) compared to LTB4 in causing degranulation of PMNL, but actually inhibits LTB4-induced degranulation of human neutrophils (Ki = 13.3 nM). However, 20-hydroxy LTB4 is as active as LTB4 in contracting parenchymal strips from guinea pig lung. 20-hydroxy LTB4 retains considerable ligand binding affinity at the BLT2 receptor, but does not appear to function as an agonist.

12(S)-HHT(12(S)-HHTrE)是通过环氧化酶（COX）的花生四烯酸代谢途径生成的脂肪酸，是BLT2的内源性配体和激动剂，12(S)-HHT BLT2轴在维持上皮组织稳态方面和炎症反应中起作用。12-HHT通过上调MKP-1抑制p38 MAPK NF-κB通路，导致UVB照射的HaCaT细胞的IL-6合成减少。

12(S)-HETE 是花生四烯酸的12-脂氧合酶代谢产物，对癌细胞增殖具有促有丝分裂作用，可增强血管紧张素 II 诱导的 BLT2 收缩（白三烯 B4小鼠动脉中 2 型受体）和 TP （血栓素受体） 介导的机制。12(S)-HETE促进动脉内皮细胞中超氧化物和异血栓素样代谢物的产生。