Alcaftadine

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). This antiallergenic agent has anti-inflammatory and mast cell stabilizing effects. 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 (Cay-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. Alcaftadine also binds to 5-HT2A and 5-HT2C receptors (Kis = 2.5 and 1.5 µM, respectively).Formal Name: 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine-3-carboxaldehyde. CAS Number: 147084-10-4. Synonyms: R-89674. Molecular Formula: C19H21N3O. Formula Weight: 307.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 284 nm. SMILES: O=CC1=CN=C2N1CCC(C=CC=C3)=C3/C2=C4CCN(C)CC\4. InChi Code: InChI=1S/C19H21N3O/c1-21-9-6-15(7-10-21)18-17-5-3-2-4-14(17)8-11-22-16(13-23)12-20-19(18)22/h2-5,12-13H,6-11H2,1H3. InChi Key: MWTBKTRZPHJQLH-UHFFFAOYSA-N.