Rupatadine (fumarate)

Rupatadine is an antagonist of histamine H1 and platelet-activating factor (PAF) receptors. It binds to rabbit platelet membranes and guinea pig cerebellum membranes with apparent Ki values of 0.55 and 0.1 µM, respectively, in radioligand binding assays. It inhibits contraction of isolated guinea pig ileum induced by histamine (pA2 = 9.29) and platelet aggregation induced by PAF in washed rabbit platelets (pA2 = 6.68). Rupatadine prevents histamine- or PAF-induced hypotension in rats (ID50s = 1.4 and 0.44 mg/kg, respectively) and reverses histamine- or PAF-induced bronchoconstriction in guinea pigs (ID50s = 113 and 9.6 mg/kg, respectively). It does not reduce locomotor activity or potentiate sleep induced by barbiturates in mice, indicating a lack of sedative effects.Formal Name: 8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, (2E)-2-butenedioate. CAS Number: 182349-12-8. Molecular Formula: C26H26ClN3 . C4H4O4. Formula Weight: 532.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. SMILES: ClC1=CC=C(/C(C2=NC=CC=C2CC3)=C4CCN(CC5=CN=CC(C)=C5)CC\4)C3=C1.OC(/C=C/C(O)=O)=O. InChi Code: InChI=1S/C26H26ClN3.C4H4O4/c1-18-13-19(16-28-15-18)17-30-11-8-20(9-12-30)25-24-7-6-23(27)14-22(24)5-4-21-3-2-10-29-26(21)25,5-3(6)1-2-4(7)8/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3,1-2H,(H,5,6)(H,7,8)/b,2-1+. InChi Key: JYBLCDXVHQWMSU-WLHGVMLRSA-N.