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Antiallergic Activity Profile in Vitro RBL-2H3 and in Vivo Passive Cutaneous Anaphylaxis Mouse Model of New Sila-Substituted 1,3,4-Oxadiazoles
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Citations
19
References
2012
Year
Antiallergic Activity ProfileAntiparasitic AgentAllergy MedicineImmunologyPharmacotherapyImmunotherapyDrug AllergyExperimental PharmacologyOxidative StressMolecular PharmacologyMedicinal ChemistryCompound 5CPharmacological StudyMouse ModelAllergyMechanism Of ActionPharmacological AgentNew Sila-substituted 1,3,4-OxadiazolesPharmacologyClinical PharmacologyNew ClassMedicineVitro Rbl-2h3Drug Discovery
A new class of sila-substituted 1,3,4-oxadiazoles was synthesized and evaluated for antiallergic activity using RBL-2H3 as the in vitro model and the in vivo anaphylactic mouse model. We observed that compound 5c effectively suppressed DNP-HSA-induced mast cell degranulation, compared to carbon analogue 9, and also suppressed the expression of TNF-α mRNA and Akt phosphorylation in antigen-stimulated RBL-2H3 cells. We also studied the effect of 5c in an in vivo passive cutaneous anaphylaxis (PCA) mouse model. The suppression by 5c was more effective than that by diphenylhydramine (DPH), a typical anti-histamine drug.
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