Leukotriene Receptor

SR2640 是一种高效且高度选择性的 LTD4/LTE4 拮抗剂，以浓度依赖性方式专一抑制LTD4引发的豚鼠回肠及气管平滑肌收缩，而不影响组胺引起的收缩反应。此化合物阻止0.4 nM [3H]LTD4与豚鼠肺组织膜受体的结合，IC50为23 nM。SR2640 使得静脉注射LTD4在豚鼠中诱发的支气管收缩剂量-效应曲线平行右移，位移程度与SR2640的剂量呈正相关。SR2640 可用于哮喘研究。

Etalocib (LY293111) sodium 作为一种口服活性的白三烯(LTB4)受体拮抗剂，对 [3H]LTB4的结合具有较强的抑制作用，其抑制常数(Ki)为25 nM。其针对LTB4诱导的钙动员的半抑制浓度(IC50)为20 nM。此外，Etalocib (LY293111) sodium 还具有诱导细胞凋亡(Apoptosis)的能力。

SB 201146 is a leukotriene B4 antagonist with high affinity.

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

12(S)-HEPE is a monohydroxy fatty acid synthesized from EPA by the action of 12-LO. Unstimulated neutrophils metabolize 12(S)-HEPE to 12(S),20-diHEPE, whereas stimulated neutrophils produce 5(S),12(S)-HEPE via the 5-lipoxygenase pathway. The competitive action of 12(S)-HEPE with arachidonic acid as a substrate for 5-LO in the formation of leukotrienes may provide a basis for the anti-inflammatory potential of ω-3 fatty acids.

SC-50605 is a second-generation LTB4 receptor antagonist.

γ-Linolenic acid ethyl ester (Ethyl γ-linolenate) 是一种白三烯 B 受体 4(LTB4)的拮抗剂，具有潜在的抗炎作用。

L 651896 是一种新型白三烯生物合成和 5-脂氧合酶抑制剂，可用于研究呼吸系统疾病和心血管疾病。

DW-1350 is an antagonist of LTB4 receptor.

Produced by neutrophils, macrophages, mast cells, and by transcellular metabolism in platelets, leukotriene C4 (LTC4) is the parent cysteinyl leukotriene formed by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4, however, is rapidly metabolized to LTD4 and LTE4, which makes the characterization of LTC4 pharmacology difficult. N-methyl Leukotriene C4 (N-methyl LTC4) is a synthetic analog of LTC4 that is not readily metabolized to LTD4 and LTE4.It acts as a potent and selective CysLT2 receptor agonist exhibiting EC50 values of 122 and > 2,000 nM at the human CysLT2 and CysLT1 receptors, respectively. It has essentially the same potency as LTC4 at both the human and murine receptors CysLT2 receptors. N-methyl LTC4 is potent and active in vivo, causing vascular leak in mice overexpressing the human CysLT2 receptor but not in CysLT2 receptor knockout mice.

Beta-Tocotrienol to serve as a new anticancer agent for treating human lung and brain cancers. It inhibits the growth of both A549 (GI50=1.38±0.334μM) and U87MG (GI50=2.53±0.604μM) cells at rather low concentrations.

KP496 is a selective, dual antagonist for Thromboxane A2 receptor and Leukotriene D4 receptor.

RG 14893 is a antagonist of high-affinity leukotriene B4 receptor.

Darbufelone (CI-1004) 是 PGF2α 和 LTB4 的非竞争性双重抑制剂。 Dabfilon 有效抑制 PGHS-2，对 PGHS-2 和 PGHS-1 的 Ki 为 10 μM，IC50 为 0.19 μM 和 20 μM。

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。

CysLT1 leukotriene receptor antagonist

HAMI 3379 (HAMI3379) 是一种选择性半胱氨酰白三烯受体2（CysLT2） 拮抗剂，以剂量和时间依赖性地减轻大鼠局灶性脑缺血后的脑损伤并抑制小胶质细胞炎症，通过抑制小胶质细胞活化来减轻缺血样神经元损伤。

Fiboflapon (GSK2190915) 是一种可口服且具有有效性 5-脂氧合酶激活蛋白 (FLAP) 抑制剂，结合 FLAP 的效价为 2.9 nM，对人血中 LTB4 有抑制作用， IC50 值为 76 nM。

LY 292728 is a highly potent antagonist of leukotriene B4 receptor.

Darbufelone mesylate (CI-1004 mesylate) 对细胞中 PGF2α 和 LTB4 产生有抑制作用。Darbufelone mesylate 对 PGHS-2 有抑制作用，IC50 值为 0.19 μM，对 PGHS-1 的IC50 值为 20 μM。

11-Keto-beta-boswellic acid 是来自乳香的一种五环三萜酸，具有抗炎活性和剂量依赖性心脏保护作用，主要是由于抑制5-脂氧合酶、白三烯、NF-κB 的激活和肿瘤坏死因子 α 的产生。

Olsalazine (Dipentium) 是一种抗炎药，用于治疗炎症性肠病。它也是一种新型的 DNA 去甲基化剂。

5-O-Demethylnobiletin (5-DEMETHYLNOBILETIN) 是从黄芪中分离出的多甲氧基黄酮，具有抗炎活性，可通过直接抑制 5-LOX 发挥作用，IC50为 0.1 μM。

Ablukast (Ro 23-3544) 是白三烯受体的选择性拮抗剂，也是LTD4受体拮抗剂。可改善 LTC4 和抗原诱导的支气管狭窄。

RG-12525（NID 525） 是一种可口服且具有选择性和竞争性的白三烯 D （LTD）拮抗剂，对 LTC4，LTD4 和 LTE4 诱导的豚鼠薄壁带收缩有抑制作用，IC50 值分别为 2.6 nM，2.5 nM 和 7 nM。RG-12525 对 CYP3A4 有抑制作用， Ki 值为 0.5 µM。RG-12525 是一种新型高效的 PPAR-γ 激动剂（IC50 值约为 60 nM），具有物种特异性，可用于研究哮喘。

U75302 is an antagonist of thymosin beta-4 (TB4) receptor with a Ki value of 159 nM on guinea pig lung membranes.

Pranlukast hemihydrate (ONO-1078 hemihydrate) 是一种具有选择性和高效性的白三烯 （LT）拮抗剂，具有抗哮喘活性，抑制 [3H]LTD4 和 [3H]LTE4 与肺膜的结合，拮抗 LTC4 诱导的豚鼠气管收缩。Pranlukast hemihydrate 可用于研究哮喘。

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.

Montelukast (Singular) 是可口服的半胱氨酸白三烯受体1 选择性拮抗剂，可用于研究预防哮喘和肝损伤。它还可减少心脏损伤，在肠缺血-再灌注损伤中也具有抗氧化作用。

LTF4 is a cysteinyl-leukotriene produced in vitro, but not reported to date in vivo. It is formed by the incubation of LTE4 with γ-glutamyl transpeptidase and glutathione. LTF4 is a weak agonist in its ability to contract vascular smooth muscle. [1] The rank order of potency of the cysteinyl-leukotrienes to contract vascular smooth muscle is LTD4 > LTC4 > LTE4 >> LTF4. [1] [2]

LTB4 antagonist 3 (compound 24e)为一种具有抗炎活性的LTB4拮抗剂，其IC50为477 nM。

LY210073 is an antagonist of the Leukotriene B4 (LTB4) receptor (IC50: 6.2 nM).

CI-949 is an allergic mediator release inhibitor, which inhibits leukotriene C4/D4 (LTC4/LTD4), histamine, and thromboxane B2 (TXB2) release (IC50s: 0.5 μM, 11.4 μM and 0.1 μM).

BIIL-260 hydrochloride 是一种具口服活性和高效性的白三烯 B(4) 受体 (LTB4) 拮抗剂，具有抗炎活性，以可饱和、可逆和竞争的方式与 LTB（4） 受体相互作用，抑制 LTB（4） 诱导的人中性粒细胞细胞内 Ca（2+） 释放 。

Quinotolast sodium inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner in the concentration range of 1-100 μg/mL.

LY 203647 is a antagonist of leukotriene D4 and E4 receptor.