blt1

BLT-1 是一种氨基硫脲铜螯合剂，是一种选择性清除受体 B1 型 (SR-BI) 抑制剂，抑制高密度脂蛋白 (HDL) 和 SR-BI 介导的细胞之间的脂质转移。

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.

BIIL 260 is a leukotriene B4 (BLT1) receptor antagonist with anti-inflammatory activity.

ZK-158252 is a selective antagonist of BLT1 receptor.

(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage of the area at risk in a canine model of ischemia-reperfusion injury induced by left anterior descending coronary artery (LAD) occlusion when administered at a dose of 0.128 mg kg prior to occlusion or reperfusion.[5] Reference：[1]. Chacos, N., Falck, J.R., Wixtrom, C., et al. Novel epoxides formed during the liver cytochrome P-450 oxidation of arachidonic acid. Biochem. Biophys. Res. Commun. 104(3), 916-922 (1982).[2]. Oliw, E.H., Guengerich, F.P., and Oates, J.A. Oxygenation of arachidonic acid by hepatic monooxygenases. Isolation and metabolism of four epoxide intermediates. J. Biol. Chem. 257(7), 3771-3781 (1982).[3]. Jiang, J.-X., Zhang, S.-J., Xiong, Y.-K., et al. EETs attenuate ox-LDL-induced LTB4 production and activity by inhibiting p38 MAPK phosphorylation and 5-LO BLT1 receptor expression in rat pulmonary arterial endothelial cells. PLoS One 10(6), e0128278 (2015).[4]. Oltman, C.L., Weintraub, N.L., VanRollins, M., et al. Epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids are potent vasodilators in the canine coronary microcirculation. Circ. Res. 83(9), 932-939 (1998).[5]. Nithipatikom, K., Moore, J.M., Isbell, M.A., et al. Epoxyeicosatrienoic acids in cardioprotection: Ischemic versus reperfusion injury. Am. J. Physiol. Heart Circ. Physiol. 291(2), H537-H542 (2006).

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.

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.

20-Carboxy-Leukotriene B4 (20-COOH LTB4) 是 Leukotriene B4 (LTB4) 的代谢物。20-Carboxy-Leukotriene B4 以高亲和力与 BLT1 受体结合。20-Carboxy-Leukotriene B4 抑制 LTB4 介导的中性粒细胞反应，迁移、脱粒、白三烯生物合成。

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。

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.