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Olopatadine hydrochloride (Opatanol) is a histamine blocker and mast cell stabilizer with an IC50 of 559 uM for the release of histamine. Evaluation of the interaction of olopatadine with histamine receptors revealed a relatively high affinity for the H1 receptor (Ki = 31.6 nM, pKi = 7.5 ?0.1) but lower affinities for H2 receptors (Ki = 100 uM, pKi = 4.0 ?0.19) and H3 receptors (Ki = 79.4 uM, pKi = 4.1 ?0.16,). The H1 selectivity of olopatadine was superior to that of other ocularly used anti-histamines studied, such as ketotifen, levocabastine, antazoline and pheniramine. It can be used in studies related to allergic conjunctivitis and rhinitis.
| Molecular Weight | 373.87 |
| Formula | C21H23NO3.HCl |
| CAS Number | 140462-76-6 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histamine Receptor Products |
|---|
| Ciproxifan maleate
Ciproxifan is an orally bioavailable, extremely potent histamine H3 inverse agonist/antagonist. |
| Antazoline hydrochloride
Antazoline hydrochloride is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. |
| Azacyclonol
Azacyclonol, also known as γ-pipradol, which diminishes hallucinations in psychotic individuals. |
| Azatadine dimaleate
Azatadine dimaleate is an antihistamine and anticholinergic compound with IC50 of 6.5nM and 10nM, respectively. |
| Bepotastine Besilate
Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
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