A histamine H1 and PAF receptor antagonist; binds to rabbit platelet membranes and guinea pig cerebellum membranes (apparent Kis = 0.55 and 0.1 µM

Rupatadine (fumarate) – 500 mg

Brand:
Cayman
CAS:
182349-12-8
Storage:
-20
UN-No:
Non-Hazardous - /

Rupatadine is an antagonist of histamine H1 and platelet-activating factor (PAF) receptors.{46659} 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.  

 

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Description

A histamine H1 and PAF receptor antagonist; binds to rabbit platelet membranes and guinea pig cerebellum membranes (apparent Kis = 0.55 and 0.1 µM, respectively, in radioligand binding assays); inhibits histamine-induced contraction of isolated guinea pig ileum (pA2 = 9.29) and PAF-induced platelet aggregation in washed rabbit platelets (pA2 = 6.68); prevents histamine- or PAF-induced hypotension in rats (ID50s = 1.4 and 0.44 mg/kg, respectively); reverses histamine- or PAF-induced bronchoconstriction in guinea pigs (ID50s = 113 and 9.6 mg/kg, respectively)

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

Synonyms: 

Molecular weight: 532

CAS: 182349-12-8

Purity: ≥98%

Formulation: A crystalline solid

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