cyslt2

HAMI 3379 is a potent and selective antagonist of the Cysteinyl leukotriene (CysLT2) receptor. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury. It also attenuates microglia-related inflammation.

Gemilukast（ONO-6950） 是一种具有口服活性和有效性的半胱氨酰白三烯 1 和 2 受体 (CysLT1 和CysLT2) 双重抑制剂，抑制 LTC 4 诱导的支气管收缩，对人 CysLT1 和 CysLT2 有抑制作用，可用于治疗哮喘。

Quininib is a regulator of Ocular Angiogenesis. Quininib significantly inhibits angiogenic tubule formation in HMEC-1 cells, angiogenic sprouting in aortic ring explants and retinal revascularisation in OIR mice.

BAY-u 9773 是 CysLT 受体(半胱氨酸白三烯受体)的非选择性拮抗剂，对于 CysLT1和 CysLT2的 IC50值大致相同，用于抑制白三烯反应。

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.

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。

ONO-4310321 is a potent, orally available dual CysLT1 and CysLT2 receptor antagonist.

ONO-2050297 is the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.

S-Geranylgeranyl-L-glutathione是孤儿G蛋白偶联受体（GPCR）P2RY8的配体。该化合物在100 nM浓度下，选择性地诱导P2RY8而非鞘氨醇-1-磷酸受体2（S1P2）、GPR55、半胱氨酸白三烯受体1（CysLT1 receptor）以及CysLT2 receptor的内吞作用。在10 nM浓度下，S-Geranylgeranyl-L-glutathione抑制了表达P2RY8的WEHI-231 B细胞淋巴瘤细胞和分离的人扁桃体生发中心B细胞由趋化因子（C-X-C motif）配体12（CXCL12）诱导的迁移。