富马酸卢帕他定

  • 化学数据
CAS号 182349-12-8 货号 BCP05230
中文名 富马酸卢帕他定
英文名 Rupatadine fumarate
中文别名
英文别名 UR-12592 Fumarate;UR12592 Fumarate;UR 12592 Fumarate; Rupafin; Alergoliber; Rinialer; Pafinur; Rupax; Ralif;
分子式 C26H26ClN3.C4H4O4 分子量 532.03
  • 用途
生物活性 Rupatadine inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors. Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA2 = 9.29 ± 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4(LTD4). It also competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2= 6.68 ± 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation. [1] In another study, it is reported rupatadine and loratadine shows similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibits inhibitory effect against TNF-α.
上下游产品 158876-82-5(卢帕他定)
信号通路 Neuro Signaling Pathway GPCR/G Protein 
靶 点 5 HT Receptor/Serotonin Receptor 

结构式

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