A H1 histamine receptor antagonist (IC50 = 8.6 nM) with anti-inflammatory and mast cell stabilizing effects; reduces edema and erythema in a guinea pig model of allergic conjunctivitis (ED50 = 0.1 mg/kg); has been used in clinical formulations in eye drops for treatment of ocular itching associated with allergic conjunctivitis

Alcaftadine – 25 mg

Brand:
Cayman
CAS:
147084-10-4
Storage:
-20
UN-No:
Non-Hazardous - /

Alcaftadine is a potent antagonist of the H1 histamine receptor (IC50 = 8.6 nM) with lower affinities for the H2 and H4 receptors (IC50s = 62 nM and 4.4 μM, respectively).{34359} This antiallergenic agent has anti-inflammatory and mast cell stabilizing effects.{34330} Alcaftadine has been shown to reduce edema and erythema in a guinea pig model of allergic conjunctivitis (ED50 = 0.1 mg/kg) more effectively than ketotifen (Item No. 20303) (ED50 = 1.0 mg/kg) and has been used in clinical formulations in eye drops for treatment of ocular itching associated with allergic conjunctivitis.{34359,34360} Alcaftadine also binds to 5-HT2A and 5-HT2C receptors (Kis = 2.5 and 1.5 μM, respectively).{34359}  

 

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Description

A H1 histamine receptor antagonist (IC50 = 8.6 nM) with anti-inflammatory and mast cell stabilizing effects; reduces edema and erythema in a guinea pig model of allergic conjunctivitis (ED50 = 0.1 mg/kg); has been used in clinical formulations in eye drops for treatment of ocular itching associated with allergic conjunctivitis

Formal name: 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine-3-carboxaldehyde

Synonyms:  R-89674

Molecular weight: 307.4

CAS: 147084-10-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity

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