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编 号：F189120
分子式：C26H26ClN3
分子量：415.96
分子式：C26H26ClN3
分子量：415.96
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CAS No: 158876-82-5
产品详情
生物活性：
Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria.
体内研究：
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.Animal Model:Male C57BL/6J mice (18 g, 6-8 wk)
Dosage:1.5, 3, 6 mg/kg
Administration:Oral gavage once a day
Result:Markedly decreased the BLM-enhanced inflammatory scores and lung index.
体外研究：
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%.
Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria.
体内研究：
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.Animal Model:Male C57BL/6J mice (18 g, 6-8 wk)
Dosage:1.5, 3, 6 mg/kg
Administration:Oral gavage once a day
Result:Markedly decreased the BLM-enhanced inflammatory scores and lung index.
体外研究：
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%.
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