中文名 | 半水普仑司特 |
英文名 | N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)benzamide hemihydrate |
别名 | 普仑司特 半水普仑司特 普仑司特水合物 普鲁司特 水合物 普鲁司特半水合物 |
英文别名 | Onon Ultair RS-411 Ono-1078 SB-205312 Ono-RS-411 Pranlukast hydrate PRANLUKASTHEMIHYDRATE Ono-1070(monoNa salt) Pranlukast Hemihydrate N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phe... 8-[4(4-phenylbutoxy)benzoyl]amino-2-(5-tetrazolyl)-4-oxo-4H-1-benzopyran N-[4-oxo-2-(2H-tetrazol-5-yl)chromen-8-yl]-4-(4-phenylbutoxy)benzamide,hydrate N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)benzamide hemihydrate N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-benzamide hemihydrate |
CAS | 150821-03-7 |
化学式 | C27H25N5O5 |
分子量 | 499.53 |
InChI | InChI=1/2C27H23N5O4.H2O/c2*33-23-17-24(26-29-31-32-30-26)36-25-21(23)10-6-11-22(25)28-27(34)19-12-14-20(15-13-19)35-16-5-4-9-18-7-2-1-3-8-18;/h2*1-3,6-8,10-15,17H,4-5,9,16H2,(H,28,34)(H,29,30,31,32);1H2 |
溶解度 | DMSO: ≥ 10 mg/mL |
存储条件 | -20°C |
外观 | 白色固体 |
体外研究 | In the radioligand binding assay, Pranlukast (ONO-1078) inhibits [ 3 H]LTE 4 , [ 3 H]LTD 4 , and [ 3 H]LTC 4 bindings to lung membranes with K i s of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. The antagonism of Pranlukast against [ 3 H]LTD 4 binding is competitive. In functional experiments, Pranlukast shows competitive antagonism against the LTC 4 - and LTD 4 -induced contractions of guinea pig trachea and lung parenchymal strips with a pA 2 range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC 4 to LTD 4 , Pranlukast also antagonizes the LTC 4 -induced contraction of guinea pig trachea (pA 2 =7.78). Pranlukast significantly reverses the LTD 4 -induced prolonged contraction without effect on the KCl- and BaCl 2 -induced contractions of guinea pig trachea. Oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT 1 receptors is inhibited by pretreatment with the CysLT 1 receptor antagonist Pranlukast (10 μM). Pranlukast protects endothelial cells against ischemia-like injury. The effects of the CysLT 1 receptor antagonist Pranlukast and the 5-lipoxygenase inhibitor Zileuton on translocation are also assessed. The results show that Pranlukast, but not Zileuton, inhibits the translocation of the CysLT 1 receptor 6 h after OGD. |
体内研究 | Carrageenan (CAR, 5 mg per mouse) is injected i.p. 24 h before LPS (50 p,g per mouse) is injected i.v. Various doses of Pranlukast (ONO-1078; 40, 20, and 10 mmol/kg), AA-861 (20, 10, and 5 mmol/kg), Indomethacin (40 mmollkg), and the controls are injected s.c. into mice 30 min before they are challenged with 50 p,g of LPS. The maximum soluble doses are 0.6 mmol/mL in 10% DMSO for AA-861 and 1.2 mmol/mL in 10% ethanol for Pranlukast. These solutions are used as the maximum doses for the treatments. The mortality of mice is significantly decreased in AA-861- Pranlukast-treated mice relative to that in the control mice. Pretreatment with CAR (5 mg i.p.) renders the mice more sensitive to the effect of LPS. Although the survival rate of mice treated with each solvent is 20% at 72 h after LPS (50 p,g per mouse) administration, s.c. treatment with AA-861 (20 mmol/kg) or Pranlukast (40 mmol/kg) significantly increases the survival rate after the LPS administration (AA-861, P<0.001; Pranlukast, P<0.01). |
危险品标志 | Xn - 有害物品 |
风险术语 | R22 - 吞食有害。 R36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36/37 - 穿戴适当的防护服和手套。 |
WGK Germany | 3 |
Hazard Class | IRRITANT |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.019 ml | 5.097 ml | 10.193 ml |
5 mM | 0.204 ml | 1.019 ml | 2.039 ml |
10 mM | 0.102 ml | 0.51 ml | 1.019 ml |
5 mM | 0.02 ml | 0.102 ml | 0.204 ml |
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