A histamine H1 and PAF receptor antagonist
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Rupatadine (fumarate)

Item No. 29478

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO: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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    50 mg

    $169

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    100 mg

    $303

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    250 mg

    $629

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    500 mg

    $1,086

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    Product Description

    Rupatadine is an antagonist of histamine H1 and platelet-activating factor (PAF) receptors.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Merlos, M., Giral, M., Balsa, D., et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J. Pharmacol. Exp. Ther. 280(1), 114-121 (1997).