Pranlukast hemihydrate (ONO-1078 hemihydrate) 是一种高效的竞争性的选择性 leukotriene 拮抗剂。Pranlukast 抑制 [³H]LTE₄，[³H]LTD₄ 和 [³H]LTC₄ 与肺膜结合，K_i 分别为 0.63±0.11，0.99±0.19 和 5640±680 nM。

Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [H]LTE 4 , [H]LTD 4 , and [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.

Solid

LTE4 0.63 nM (Ki) LTD4 0.99 nM

In the radioligand binding assay, Pranlukast (ONO-1078) inhibits [H]LTE4, [H]LTD4, and [H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. The antagonism of Pranlukast against [H]LTD4 binding is competitive. In functional experiments, Pranlukast shows competitive antagonism against the LTC4- and LTD4-induced contractions of guinea pig trachea and lung parenchymal strips with a pA2 range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC4 to LTD4, Pranlukast also antagonizes the LTC4-induced contraction of guinea pig trachea (pA2=7.78). Pranlukast significantly reverses the LTD4-induced prolonged contraction without effect on the KCl- and BaCl2-induced

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 (

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Obata T, et al. In vitro antagonism of ONO-1078, a newly developed anti-asthma agent, against peptide leukotrienes in isolated guinea pig tissues. Jpn J Pharmacol. 1992 Nov;60(3):227-37.
[2]. Fang SH, et al. Nuclear translocation of cysteinyl leukotriene receptor 1 is involved in oxygen-glucose deprivation-induced damage to endothelial cells. Acta Pharmacol Sin. 2012 Dec;33(12):1511-7.

In Vitro: DMSO : 25 mg/mL (50.97 mM; Need ultrasonic)H₂O : 1 mg/mL (2.04 mM; ultrasonic and warming and heat to 80°C)配制储备液