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Rupatadine

CAS No. : 158876-82-5

MCE 站：Rupatadine

产品活性：Rupatadine (UR-12592) 是一种有效的，具有口服活性的长效 PAF/H1 受体的双抑制剂，K_i 值分别为 0.55 μM 和 0.1 μM。Rupatadine 可用于过敏性鼻炎和荨麻疹的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation  |  Autophagy

作用靶点：Histamine Receptor  |  Autophagy

In Vitro: Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA₂=9.29) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4).
Rupatadine competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA₂=6.68) and in human platelet-rich plasma (HPRP) (IC₅₀=0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation.
Rupatadine (0.1-30 μM) inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%.

In Vivo: Rupatadine blocks histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID₅₀=1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID₅₀=113 and 9.6 μg/kg i.v.).
Rupatadine potently inhibits PAF-induced mortality in mice (ID₅₀=0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID₅₀=1.6 and 0.66 mg/kg i.v.).
Rupatadine (6 mg/kg) promotes the absorption of the lesions and decreased the density of lungs.

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