leukotriene d-4

Leukotriene D4 (LTD4) 是一种由花生四烯酸形成的强效促炎介质，是一种支气管收缩剂，可诱导成骨细胞衰老。Leukotriene D4 诱导潜在致癌基因的转录活性，可用于研究哮喘。

RS-601 是一种有效的 leukotriene D4/thromboxane A2 双重抑制剂，对抗原诱导的气道高反应性 （AHR）有抑制作用且在豚鼠哮喘模型中显示出平喘作用。

ONO4057 是一种具有有效性和口服活性的 Leukotriene B4 受体拮抗剂，其 IC50 值为 0.7±0.3 μM。 ONO4057 对大鼠同种异体移植的免疫抑制作用。

14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both guinea pig ileum and pulmonary parenchyma in contrast to the effects of 5-LO-derived LTs. However, in an in vitro permeability assay, 14,15-LTD4 can increase vascular permeability of human endothelial cell monolayers, with similar potency to that of 5-LO-derived LTs, resulting in plasma leakage, a hallmark of inflammation.

11-trans Leukotriene D4 (11-trans LTD4) is a C-11 double bond isomer of LTD4. LTD4 undergoes slow temperature-dependent isomerization to 11-trans LTD4 during storage. 11-trans LTD4 retains about 10-25 % of the potency for contraction of guinea pig ileum, trachea and parenchyma compared to LTD4. It exhibits an ED50 ranging between 12-60 nM for contraction of guinea pig trachea.

Leukotriene D4-d5 是 Leukotriene D4 的氘代物。Leukotriene D4 是一种由 γ-谷氨酰转肽酶代谢 LTC4 形成的过敏反应慢反应物质 (SRS-A) 的重要成分。它是 LTC4 的第一个半胱氨酸-白三烯代谢产物。Leukotriene D4 所引发的支气管收缩以及增加的血管通透性与哮喘的发病机制和急性过敏反应密切相关。

Pobilukast (SKF 104353) 是一种选择性半胱氨酰白三烯受体拮抗剂，可阻断磷脂酰肌醇代谢和白三烯D诱导的血栓素合成，可用于研究过度心肌再灌注损伤 （MI/R） 大鼠限制心肌损伤。

Parogrelil Free Base (NM-702 Free Base) 是一种选择性磷酸二酯酶3抑制剂，具有支气管扩张和抗炎作用，抑制白三烯（LT）D（4）和组胺诱导的离体豚鼠气管条的收缩，可用于研究支气管哮喘。

Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of 5 mM.2,3Olsalazine (150 mg/kg for 8 days) improves stool consistency and decreases occult and gross bleeding as well as myeloperoxidase (MPO) activity and leukotriene B4levels in colon tissue in a mouse model of acute colitis induced by dextran sulfate .4Olsalazine also inhibits bovine xanthine oxidasein vitro(IC50= 3.4 mg/L) and lowers serum uric acid levels in a mouse model of hyperuricemia induced by oxonic acid when administered at a dose of 20 mg/kg.5Formulations containing olsalazine have been used in the treatment of inflammatory bowel disease (IBD) and ulcerative colitis. 1.Nugent, S.G., Kumar, D., Rampton, D.S., et al.Intestinal luminal pH in inflammatory bowel disease: Possible determinants and implications for therapy with aminosalicylates and other drugsGut48(4)571-577(2001) 2.Pamukcu, R., Hanauer, S.B., and Chang, E.B.Effect of disodium azodisalicylate on electrolyte transport in rabbit ileum and colon in vitro. Comparison with sulfasalazine and 5-aminosalicylic acidGastroenterology95(4)975-981(1988) 3.Mohsen, A.Q.M., Mulvey, D., Priddle, J.D., et al.Effects of olsalazine in the jejunum of the ratGut28(3)346-352(1987) 4.Murthy, S., Murthy, N.S., Coppola, D., et al.The efficacy of BAY y 1015 in dextran sulfate model of mouse colitisInflamm. Res.46(6)224-233(1997) 5.Niu, Y., Li, H., Gao, L., et al.Old drug, new indication: Olsalazine sodium reduced serum uric acid levels in mice via inhibiting xanthine oxidoreductase activityJ. Pharmacol. Sci.135(3)114-120(2017)