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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Histamine Receptor Products |
|---|
| Peptide 401
Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT). |
| Granuliberin R
Granuliberin R is a new mast cell degranulating peptide comes from amphibian, can be isolated from the skin of frog Rana rugosa. |
| Dimethindene maleate
Dimethindene maleate is a selective histamine H1 receptor antagonist with antihistamine activity.Dimethindene maleate may be used in studies related to allergic reactions. |
| 4-Methylhistamine
4-Methylhistamine is a potent agonist of histamine 4 receptor (H4R). |
| H4R antagonist 3
H4R antagonist 3 is a histamine-4 receptor antagonist with an EC50 of ＜10 mM. |
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