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Cellagentech/Alcaftadine | Histamine (H1/H4) receptor antagonist/C2522-5/5 mg (powder)

  
  2024-04-28
  
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[8.4.0.0(3,7)]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.


Reference:

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.

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