Biochem/physiol Actions
Rupatadine (UR-12592) is an orally active, dual histamine H1 and platelet-activating factor (PAF) receptor antagonist (Ki(app) = 100/550 nM against pyrilamine/WEB2086 binding to guinea pig cerebellum/rabbit platelet membranes) that inhibits histamine-induced guinea pig ileum contraction (pA2 = 9.29) and PAF-induced platelet aggregation (IC50 = 0.68 μM/human PRP). Rupatadine blocks histamine-/PAF-induced hypotension (ID50 = 1.4/0.44 mg/kg i.v. rats) and bronchoconstriction (ID50 = 113/9.6 μg/kg i.v. guinea pigs), as well as prevents mortality caused by PAF (ID50 = 0.31 mg/kg i.v. or 3.0 mg/kg p.o. mice) and endotoxin (mice/rats ID50 = 1.6/0.66 mg/kg i.v.) in vivo.
- UPC:
- 51173100
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- SML2898-10MG
- CAS:
- 182349-12-8