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Description: Rupatadine (also known as UR-12592) is a potent inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. 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 uM), while not affecting ADP- or arachidonic acid-induced platelet aggregation.
References: J Pharmacol Exp Ther. 1997 Jan; 280(1):114-21.
Related CAS#: 158876-82-5 (free base); 182349-12-8 (Fumarate)
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