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(Rac)-Modipafant

(Rac)-Modipafant用途

(Rac)-Modipafant (UK-74505) 是一种口服的、选择性的、长效的不可逆血小板活化因子受体 (PAFR) 受体拮抗剂。(Rac)-Modipafant 预防严重登革热感染。

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(Rac)-Modipafant名称

[ CAS 号 ]:
122956-68-7

[ 英文名 ]:
(Rac)-Modipafant

[英文别名 ]:

(Rac)-Modipafant生物活性

[ 描述 ]:

(Rac)-Modipafant (UK-74505) 是一种口服的、选择性的、长效的不可逆血小板活化因子受体 (PAFR) 受体拮抗剂。(Rac)-Modipafant 预防严重登革热感染。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[体内研究]

(Rac)-莫迪帕凡特(UK-74505)(10 mg/kg；p.o.；每天两次,直至第10天)可预防严重的登革热感染[3]。(Rac)-Modipafant对PAF诱导的兔洗涤血小板聚集具有高度选择性和时间依赖性的抑制作用(预孵育0.25和60分钟后,IC50分别为26.3和1.12 nM)[4]。(Rac)-莫迪帕芬(5-20 mg/kg；p.o.)剂量依赖性地抑制酵母多糖诱导的关节痛过敏[5]。动物模型：8至10周龄BALB/c小鼠(DEN-2株感染)[3]剂量：10mg/kg给药：P.o.；每天两次(从第0、3、5或7天开始)到第10天结果：与DEN-2感染相关的致死率降低了约50%。动物模型：雄性BALB/C(8～10周龄)野生型小鼠[5]剂量：5,10,20mg/kg给药：P.o.结果：剂量依赖性抑制酵母多糖引起的关节痛敏。

[参考文献]

[1]. O'Connor BJ, et al. Inhibitory effect of UK,74505, a potent and specific oral platelet activating factor (PAF) receptor antagonist, on airway and systemic responses to inhaled PAF in humans. Am J Respir Crit Care Med. 1994;150(1):35-40.

[2]. Alabaster VA, et al. UK-74,505, a novel and selective PAF antagonist, exhibits potent and long lasting activity in vivo. Agents Actions Suppl. 1991;34:221-227.

[3]. Parry MJ, Alabaster VA, et al. Pharmacological profile of UK-74,505, a novel and selective PAF antagonist with potent and prolonged oral activity. J Lipid Mediat Cell Signal. 1994;10(3):251-268.

[4]. Souza DG, et al. Essential role of platelet-activating factor receptor in the pathogenesis of Dengue virus infection. Proc Natl Acad Sci U S A. 2009;106(33):14138-14143.

[5]. Guerrero AT, et al. The role of PAF/PAFR signaling in zymosan-induced articular inflammatory hyperalgesia [published correction appears in Naunyn Schmiedebergs Arch Pharmacol. 2013 Apr;386(4):351. Zaperlon, Ana C [corrected to Zarpelon, Ana C]]. Naunyn Schmiedebergs Arch Pharmacol. 2013;386(1):51-59.