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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 |
|---|
| Dimethindene
Dimethindene is a potent, selective histamine H1 antagonist. |
| ABT-288
ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. |
| A-349821
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. |
| Betazole
Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active histamine H2 receptor agonist. |
| Tiotidine
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). |
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