mediator release

Quazolast (RHC 3988) 是一种有效的介质释放抑制剂，是对豚草抗原鼻腔挑战的对照。Quazolast 在防止猪笼草鼻腔挑战后的鼻塞和鼻痒方面优于安慰剂。

Eclazolast (RHC 2871) 是一种亲脂性抗过敏化合物，在肥大细胞模型中抑制介质释放。Eclazolast 通过在细胞内只影响与Fc(epsilon)RI 相关的直接过程而抑制细胞外分泌。Eclazolast 的效果高度依赖于触发细胞的抗原浓度。

Salbutamol (Albuterol) 是短效的 β2 肾上腺素受体激动剂，用于哮喘和慢性阻塞性肺疾病(COPD) 引发的支气管痉挛的研究。

PTZ-343 是一种鲁米诺的强效发光增强剂 (enhancer)。它极大的增强了过氧化物酶催化的鲁米诺化学发光氧化反应 (>80%) 的光输出。

Tranilast (SB 252218) 是一种抗过敏药物，可抑制炎症细胞释放脂质介质和细胞因子，抑制前列腺素 D2 (PGD2)产生，IC50为 0.1 mM。它拮抗血管紧张素 II 并抑制其在血管平滑肌细胞中的生物学作用，具有抗炎和免疫调节作用。

Emedastine (LY188695) 是一种可口服的，选择性和高亲和力的组胺 H1受体拮抗剂，Ki 值为 1.3 nM。它是苯并咪唑衍生物，可用于过敏性鼻炎、过敏性皮肤疾病和过敏性结膜炎的研究。

Bradykinin 是由激肽释放酶-激肽系统产生的活性肽。 它是炎症调节因子和神经调节因子，对几种血管和肾功能也有调节作用。

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).

GSK-5498A is a selective blocker of CARC (IC50, 1 μM). It inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.

Repirinast is a mediator release inhibitor. It is used to treat asthma.

ISOCROMIL，一种色酮类化合物，具有抗过敏作用。它作为介质释放抑制剂，在被动皮肤过敏反应治疗中以及用作抗哮喘化合物方面，发挥着重要作用。

Ro 19-1400, a platelet-activating factor antagonist, directly inhibits immunoglobulin E-dependent mediator release.

CI 922 is an anaphylaxis mediator release inhibitor. It inhibits the activation of human neutrophils.

Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂，IC50为6.0 nM。

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

Acetylshikonin 来源于紫草根，具有抗癌、抗炎作用。它是一种 AChE 抑制剂，具有很强的抗凋亡活性。它是一种非选择性的细胞色素 P450抑制剂，对所有 P450 亚型抑制的 IC50值范围为 1.4-4.0 μM。

Nivimedone Free Base inhibits mediator release & capillary permeability.

Picumast dihydrochloride is a prophylactically active anti-allergic compound which combines inhibition of mediator release and action. The activity profile of PDH differs clearly from that of known prophylactic anti-allergic drugs such as DSCG and ketotifen.

HPR-611 is a potent inhibitor of anaphylactic chemical mediator release.

Tylogenin, a steroidal aglycone generated by acid hydrolysis from two seasonal glycosides occurring in Tylophora sylvatica, inhibits IgE-induced basophil mediator release for allergic reactions. In the rabbit basophil-dependent serotonin release (BDSR) assay system, the inhibitory activity of tylogenin was significantly greater than that of its parent glycosides, tylophoroside and acetyltylophoroside, and that of dexamethasone. The activity of tylogenin was found to increase with the incubation time. In the human leukocyte-dependent histamine release test model, the glycosides had only a minimal activity. In contrast, tylogenin, with a geom mean IC50 = 49 microM, exerted a significantly greater potency than dexamethasone. These results suggest that tylogenin could represent a new class of antiallergic agents.

Salbutamol-d9 是 Salbutamol 的氘代化合物。Salbutamol 的 CAS 号为 18559-94-9。Salbutamol 是短效的 β2 肾上腺素受体激动剂，用于哮喘和慢性阻塞性肺疾病 (COPD) 引发的支气管痉挛的研究。

Salbutamol-d3 是 Salbutamol 的氘代化合物。Salbutamol 的 CAS 号为 18559-94-9。Salbutamol 是短效的 β2 肾上腺素受体激动剂，用于哮喘和慢性阻塞性肺疾病 (COPD) 引发的支气管痉挛的研究。

2'-Hydroxydaidzein 是一种在植物中发现的异黄酮类植物素，是一种天然化合物。2'-Hydroxydaidzein 具有抗氧化活性，主要由o -氢键解离焓(BDE)和氢原子转移(HAT)机制驱动。2'-Hydroxydaidzein 抑制炎症细胞中的化学介质，可能对治疗和预防与化学介质产生过多有关的中枢和外周炎症性疾病有作用。2'-Hydroxydaidzein 对大鼠中性粒细胞和formyl-Met-Leu-Phe cytochalasin B（fMLP CB）的释放具有抑制作用，IC（50）值分别为2.8+ -0.1和5.9+ -1.4 microM。

Pd-C-II has anti-inflammation activity, it can inhibit TNF-α production and iNOS protein expression and inhibit COX-2 protein expression in LPS-stimulated RAW 264.7 cells. Pd-C-II inhibits anaphylactic mediator release from purified mast cells induced by