product name Olopatadine HCl
Description: Olopatadine HCl is a second-generation histamine H1 receptor antagonists and a mast cell stabilizer with an IC50 of 559 μM for the release of histamine. Olopatadine HCl is used to treat itching associated with allergic conjunctivitis (eye allergies). There is also a potential for Olopatadine as a treatment modality for steroid rebound (red skin syndrome). Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials
References: Expert Opin Drug Metab Toxicol. 2011 Dec;7(12):1593-9.
373.87
Formula
C21H23NO3.HCl
CAS No.
140462-76-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 75 mg/mL (200.6 mM)
Water: 13 mg/mL (34.8 mM)
Ethanol: 8 mg/mL (21.39 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427257
| In Vitro |
In vitro activity: Olopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively). Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Pharmacology. 2005 Dec;75(1):45-52; Jpn J Pharmacol. 2002 Apr;88(4):379-97. |
