Rupatadine  (Synonyms: UR-12592)

Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with K_is of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria^[1][2][3].

Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA₂=9.29) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4)^[1].
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^[1].
Rupatadine (0.1-30 μM) inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.)^[1].
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.)^[1].
Rupatadine (6 mg/kg) promotes the absorption of the lesions and decreased the density of lungs^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

415.96

C₂₆H₂₆ClN₃

158876-82-5

CC1=CN=CC(CN2CC/C(CC2)=C3C4=CC=C(Cl)C=C4CCC5=CC=CN=C5\3)=C1

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• [1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21.  [Content Brief]

  [2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60.  [Content Brief]

  [3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631.  [Content Brief]