Olopatadine HCl

Histamine blocker CAS# 140462-76-6

Olopatadine HCl

Catalog No. BCC4545----Order now to get a substantial discount!

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Chemical structure

Olopatadine HCl

3D structure

Chemical Properties of Olopatadine HCl

Cas No. 140462-76-6 SDF Download SDF
PubChem ID 5282402 Appearance Powder
Formula C21H24ClNO3 M.Wt 373.87
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (133.74 mM; Need ultrasonic)
H2O : 6.67 mg/mL (17.84 mM; Need ultrasonic)
Chemical Name (Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydro-dibenz[b,e]oxepin-2-acetic acid hydrochloride
SMILES [H+].[Cl-].CN(C)CCC=C/1c2ccccc2COc3ccc(CC(O)=O)cc13
Standard InChIKey HVRLZEKDTUEKQH-NOILCQHBSA-N
Standard InChI InChI=1S/C21H23NO3.ClH/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24;/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24);1H/b18-8-;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Olopatadine HCl

DescriptionHistamine H1 receptor antagonist (Ki = 31.6 nM). Inhibits the release of histamine, prostaglandin D2 and tryptase in a concentration-dependent manner. Mast cell stabilizer; inhibits mast cell mediator release. Also suppresses inflammation by inhibition of cytokine production.

Olopatadine HCl Dilution Calculator

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Olopatadine HCl Molarity Calculator

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Preparing Stock Solutions of Olopatadine HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6747 mL 13.3736 mL 26.7473 mL 53.4945 mL 66.8682 mL
5 mM 0.5349 mL 2.6747 mL 5.3495 mL 10.6989 mL 13.3736 mL
10 mM 0.2675 mL 1.3374 mL 2.6747 mL 5.3495 mL 6.6868 mL
50 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.0699 mL 1.3374 mL
100 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.5349 mL 0.6687 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Olopatadine HCl

Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Olopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and th

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References on Olopatadine HCl

Improved quality of life among seasonal allergic rhinitis patients treated with olopatadine HCl nasal spray 0.4% and olopatadine HCl nasal spray 0.6% compared with vehicle placebo.[Pubmed:16913262]

Allergy Asthma Proc. 2006 May-Jun;27(3):202-7.

Seasonal allergic rhinitis (SAR) exerts a significant adverse impact on health-related quality of life (QoL) and productivity of those who suffer from it. Unfortunately, some therapies for SAR also have a negative impact. Therefore, it is important to scrutinize the influence of new SAR therapies on patients' QoL and ability to function. The purpose of this study was to evaluate the effect of a new nasal antihistamine, olopatadine, on QoL in SAR patients. In a multicenter, randomized, double-blind SAR study comparing olopatadine 0.6 and 0.4% to placebo nasal spray, patients completed the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) at baseline and after 2 weeks of treatment. The RQLQ is a validated questionnaire that addresses overall QoL and 7 domains of impairment associated with rhinoconjunctivitis (activities, sleep, non--nose/eye allergy symptoms, practical problems, nasal symptoms, eye symptoms, and emotional impairment). The overall RQLQ mean changes from baseline with olopatadine 0.6% (-1.1 +/- 1.4) and 0.4% (-1.1 +/- 1.3) nasal sprays were superior (p < 0.05) to placebo (-0.8 +/- 1.2). Olopatadine spray 0.6% was superior to placebo in six of the seven RQLQ domains and olopatadine 0.4% was superior to placebo in five RQLQ domains (p < 0.05). The correlation between the olopatadine 0.6% mean total symptom scores and mean RQLQ score was r = 0.66 (p < 0.0001), indicating that the enhancement in QoL derived from olopatadine therapy was significantly associated with symptom reduction. Olopatadine nasal spray is an effective antiallergy medication that significantly improves the QoL of patients suffering from SAR.

Comparison of the effects of ketotifen fumarate 0.025% and olopatadine HCl 0.1% ophthalmic solutions in seasonal allergic conjunctivities: a 30-day, randomized, double-masked, artificial tear substitute-controlled trial.[Pubmed:16291412]

Clin Ther. 2005 Sep;27(9):1392-402.

BACKGROUND: Topical antiallergic agents, such as antihistamines and mast-cell stabilizers, are the main therapeutic options for seasonal allergic conjunctivitis (SAC). Ketotifen fumarate and Olopatadine HCl have dual action that offers a combination of these 2 mechanisms. Although clinical studies comparing the efficacy of these 2 drugs have shown that both were effective in the treatment of SAC, the results were contradictory and did not include the effects of these drugs on inflammatory markers. OBJECTIVES: The aims of this study were to compare the clinical efficacy of topical ketotifen and olopatadine eye drops and to determine the effects of these 2 drugs on the expression of cell adhesion molecules (CAMs) and inflammatory markers in conjunctival surface cells in patients with SAC. METHODS: This 30-day, randomized, double-masked, artificial tear substitute (ATS)-controlled clinical trial was conducted at the Department of Ophthalmology, Karadeniz Technical University, School of Medicine, Trabzon, Turkey. Patients with SAC were included in the study and randomly assigned to 1 of 3 groups: topical ketotifen fumarate 0.025% ophthalmic solution, topical Olopatadine HCl 0.1% ophthalmic solution, or ATS (control group). All drugs were administered 2 drops per eye BID for 30 days. At the beginning of the study (day 0; baseline), on day 15, and on day 30, clinical scores (itching, tearing, redness, eyelid, swelling, and chemosis) and conjunctival impression cytology specimens were obtained. The percentages of cells expressing intercellular adhesion molecule 1, vascular CAM-1, human leukocyte antigen-DR, and beta1-integrin (CD29) from conjunctival impression cytology specimens were determined using flow cytometry. Patients were questioned about adverse events (AEs) at each visit. Ocular discomfort on installation of the drugs was recorded as an AE. RESULTS: Thirty-nine patients (20 men, 19 women; age range, 18-61 years) with SAC were included. Twelve patients received ketotifen; 13, olopatadine; and 14, ATS. In both active-treatment groups, the improvements of clinical scores (tearing and itching) were more pronounced compared with those in the ATS group, although the day-30 difference in tearing score between the olopatadine and ATS groups was not statistically significant. No significant within-group or between-group differences in mean scores for redness, chemosis, or eyelid swelling were found. The expression rates of CAMs and inflammatory markers in conjunctival surface cells were significantly more reduced with ketotifen and olopatadine compared with ATS. However, clinical and flow cytometric parameters were improved with ATS at 15 and 30 days compared with baseline. No AEs were observed during the study period. CONCLUSIONS: In this short-term study in a selected, small study population with SAC, ketotifen and olopatadine diminished the expression of CAMs and inflammatory markers on the conjunctival surface cells effectively. Both active treatments were more efficacious compared with ATS and were well tolerated.

Olopatadine ameliorates rat experimental cutaneous inflammation by improving skin barrier function.[Pubmed:17962722]

Pharmacology. 2008;81(2):118-26.

Olopatadine hydrochloride (olopatadine) is an antiallergic agent with histamine H(1) receptor antagonistic action. We investigated the possible efficacies of olopatadine on the chronic inflammatory dermatitis and the impaired skin barrier functions induced by repeated application of oxazolone in rats. Oxazolone-sensitized rats were challenged with oxazolone applied to the ear every 3 days. Olopatadine was orally administered once daily (1 and 3 mg/kg/day). The effects of the drug were quantified by measurements of ear thickness, levels of cytokines in the lesioned ear and the number of scratching episodes. As parameters of skin barrier function, transepidermal water loss (TEWL) and hyaluronic acid (HA) levels in the lesioned ear were measured. The effect of olopatadine on the production of HA by cultured dermal fibroblasts was also measured. Repeated topical application of oxazolone to rat ears induced local inflammation that was exemplified by swelling. In inflamed ears, the amount of IFN gamma increased at both the protein and mRNA level, but IL-4 levels changed minimally. Olopatadine significantly decreased ear swelling and the number of scratching episodes. The drug also significantly inhibited the increase of IFN gamma and nerve growth factor production in inflamed ears. Olopatadine significantly inhibited the increase in TEWL and the decrease in HA in lesioned ears. Furthermore, the drug stimulated the production of HA by cultured dermal fibroblasts. These results suggest that olopatadine suppressed inflammation and scratching not only by inhibiting cytokine production, but also by repairing skin barrier function.

Description

Olopatadine hydrochloride (ALO4943A) is a histamine blocker used to treat allergic conjunctivitis.

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