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Alcaftadine | Histamine (H1/H4) receptor antagonist

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Product Description

Alcaftadine, a imidazobenzazepine-based antagonist of the histamine receptors, has a pKi of 8.5 and 5.8 for the H1 receptor and H4 receptors, respectively. Additionally, Alcaftadine shows higher affinity for the H2 receptor than ketotifen. [1]

In support of its potent anti-inflammatory properties, Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects. [2] Receptor binding studies revealed less significant effects ranging from a moderate affinity for cholinergic muscarinic receptors and lower affinity for human a2A-adrenoreceptors, serotonin 5-H51A, 5-HT2A receptors, and melanocortin MC4 receptors. [2] Furthermore, displacement experiments showed that at concentrations up to 10 uM, Alcaftadine did not interact with other receptors, transporters, or ion channel binding sites, including the hERG channel. [3]

Technical information:

Chemical Formula:   C19H21N3O
CAS #:   147084-10-4
Molecular Weight:   307.38
Purity:   > 98%
Appearance:   White
Chemical Name:   2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclo[,7)]tetradeca- 1(14),3,5,10,12-pentaene-6-carbaldehyde
Solubility:   Up to 20 mM in DMSO
Synonyms:   Alcaftadine, 147084-10-4, Lastacaft

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. Gallois-Bernois et al., Alcaftadine, a new antihistamine with combined antagonist activity at histamine H1, H2, and H4 receptors. J. Receptor Ligand Channel Res. 2012, 5, 9-20.
2. Namdar et al., Alcaftadine: A topical antihistamine for use in allergic conjunctivitis. Drugs of Today, 2011, 47(12), 883-890. Pubmed ID: 22348913
3. Bohets et al., Clinical Pharmacology of Alcaftadine, a Novel Antihistamine for the Prevention of Allergic Conjunctivitis. J. Ocular. Pharm. Ther. 2011, 27(2), 187-195.

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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