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Epinastine (also known as WAL-801CL HCl) is a potent antihistamine H1 without sedative activity and a mast cell stabilizer that is used in eye drops for the treatment of allergic conjunctivitis. The release of histamine from mast cells is inhibited by epinastine hydrochloride, which also blocks the histamine H1 receptor. This avoids the common allergic reactions that result from histamine activation on the skin, mucous membranes, and capillaries.
| ln Vitro |
Epinastine can displace specific [3H]NC-5Z binding at low concentrations in locust nervous tissue. Epinastine binds to the neuronal octopamine receptor in honey bees with Ki of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain[2].
Epinastine inhibits the release of histamine from peritoneal mast cells in rats that is brought on by compound 48/80 and the antigen-antibody reaction. Comparably, epinastine inhibits the release of histamine from isolated rat peritoneal mast cells as well as from rat mesenterial pieces when compound 48/80 is present. In actively sensitized guinea pigs, epinastine effectively inhibits both the release of Ca2+ from the intracellular Ca store of rat peritoneal mast cells exposed to compound 48/80 and substance P, as well as the uptake of Ca2+ into lung mast cells[3]. One of the chemokines released by eosinophils isolated from atopic diseases, IL-8, is suppressed by epinastine in a dose- and time-dependent manner[4].
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| ln Vivo |
Epinastine demonstrates a high affinity for H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine prevents rats, dogs, and guinea pigs from experiencing histamine-induced reactions in their skin or lungs[1].
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| References |
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| Molecular Formula |
C₁₆H₁₅N₃
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|---|---|
| Molecular Weight |
249.31
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| Exact Mass |
249.13
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| Elemental Analysis |
C, 77.08; H, 6.06; N, 16.85
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| CAS # |
80012-43-7
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| Related CAS # |
Epinastine hydrochloride; 108929-04-0; Epinastine-13C,d3 hydrobromide; 127786-29-2 (HBr)
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| Appearance |
Solid powder
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| SMILES |
C1C2C3=CC=CC=C3CC4=CC=CC=C4N2C(=N1)N
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| InChi Key |
WHWZLSFABNNENI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18)
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| Chemical Name |
2,4-diazatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine
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| Synonyms |
WAL801; WAL 801; WAL-801; Epinastine; brand names Alesion, Elestat, Purivist, Relestat
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (~200.6 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0111 mL | 20.0554 mL | 40.1107 mL | |
| 5 mM | 0.8022 mL | 4.0111 mL | 8.0221 mL | |
| 10 mM | 0.4011 mL | 2.0055 mL | 4.0111 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02182518 | Completed | Drug: Epinastine Drug: Placebo |
Rhinitis, Allergic, Perennial | Boehringer Ingelheim | May 2000 | Phase 3 |
| NCT02260063 | Completed | Drug: Epinastine syrup Drug: Epinastine tablets |
Healthy | Boehringer Ingelheim | November 1998 | Phase 1 |
| NCT02182531 | Completed | Drug: Epinastine Drug: Pseudoephedrine |
Healthy | Boehringer Ingelheim | August 1999 | Phase 1 |
| NCT02260037 | Completed | Drug: Epinastine nasal Drug: Placebo |
Healthy | Boehringer Ingelheim | August 2001 | Phase 1 |
| NCT01382654 | Completed | Drug: epinastine 0.1% Drug: epinastine 0.2% |
Allergic Rhinitis | Merck Sharp & Dohme LLC | September 2006 | Phase 2 |
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