产品说明书

Pranlukast

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Chemical Structure| 103177-37-3 同义名 : 普仑司特 ;ONO-1078;ONO-RS-411;SB 205312
CAS号 : 103177-37-3
货号 : A108288
分子式 : C27H23N5O4
纯度 : 98%
分子量 : 481.503
MDL号 : MFCD00864631
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(72.69 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Pranlukast is a selective, competitive antagonist of the cysteinyl leukotrienes, leukotriene (LT) C4, LTD4 and LTE4, antagonising binding at the cysteinyl leukotriene type 1 (CysLT1) receptor. In isolated human bronchial smooth muscle preparations, pranlukast caused a concentrationdependent inhibition or reversal of LTC4-, LTD4- and house dust antigen-induced bronchial contraction, but had minimal or no effect on histamine (H)- prostaglandin F2α-, acetylcholine- or thromboxane, A2 (TXA2) mimetic agonist-induced contraction (at 37°C)[3]. In vitro , antigen-induced contraction was inhibited more effectively with pranlukast than with an H1-receptor antagonist; however, pranlukast in combination with an H1-receptor antagonist was more potent than either agent alone[4].Pranlukast has shown a range of anti-inflammatory effects on airways in animal models, including attenuation or inhibition of microvascular leakage in the trachea, bronchi and small airways,LTD4-, capsaicin- or allergen-induced eosinophilia in bronchoalveolar lavage fluid (BAL), bronchial epithelial and subepithelial tissue or lung parenchyma and the expression of mRNA for interleukin-5 in BAL cells[5]. In addition, pranlukast inhibited airway smooth muscle DNA synthesis and reduced allergen-induced airway smooth muscle cell thickness in repeatedly ovalbumin-sensitised rats[6].Animal models show that pranlukast is cleared through metabolic transformation (primarily glucuronic acid conjugation); an in vitro study indicated that the drug is metabolised via cytochrome P450 (CYP) enzymes. The main metabolites formed are mono- and dihydroxylated molecules and their glucuronide conjugates[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00127647 Rhinitis, Allergic, Seasonal Phase 3 Completed - -
NCT01539304 Perennial Allergic Rhinitis Phase 3 Completed - Korea, Republic of ... 展开 >> Seoul National University Hodpital Seoul, Korea, Republic of 收起 <<
NCT00410735 Chronic Sinusitis Phase 3 Completed - Japan ... 展开 >> Chubu region Chubu, Japan Hokuriku region Hokuriku, Japan Kanto region Kanto, Japan Kinki region Kinki, Japan Kyushu region Kyushu, Japan Tohoku region Tohoku, Japan 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.38mL

2.08mL

1.04mL

20.77mL

4.15mL

2.08mL
参考文献

[1]Ichiyama T, Hasegawa S, et al. Pranlukast inhibits NF-kappa B activation in human monocytes/macrophages and T cells. Clin Exp Allergy. 2003 Jun;33(6):802-7.

[2]Liu YC, Khawaja AM, et al. Effects of the cysteinyl leukotriene receptor antagonists pranlukast and zafirlukast on tracheal mucus secretion in ovalbumin-sensitized guinea-pigs in vitro. Br J Pharmacol. 1998 Jun;124(3):563-71.

[3] Susan J Keam,et al. Pranlukast: a review of its use in the management of asthma. Drugs. 2003;63(10):991-1019.

[4]Yamaguchi T,et al. A novel leukotriene antagonist, ONO-1078, inhibits and reverses human bronchial contraction induced by leukotrienes C4 and D4 and antigen in vitro . Am Rev Respir Dis 1992 Oct; 146 (4): 923-9.

[5]Hojo M,et al. Role of cysteinyl leukotrienes in CD4+ T cell-driven late allergic airway responses.J Pharmacol Exp Ther 2000 May; 293 (2): 410-6

[6]Salmon M,et al. Involvement of cysteinyl leukotrienes in airway smooth muscle cell DNA synthesis after repeated allergen exposure in sensitized Brown Norway rats. Br J Pharmacol 1999 Jul; 127 (5): 1151-8

[7]The Japan Pharmaceutical Manufacturers Association. Japan Pharmaceutical Reference: Onon capsules [online].