| Name | Epinastine hydrochloride |
| Description | Epinastine hydrochloride (WAL-801CL HCl) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis. |
| In vitro | Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. [1] Epinastine is able to displace specific [3H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with Ki of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain. [2] Epinastine causes an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine is similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Epinastine is effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P. [3] Epinastine shows a dose- and time-dependent suppressive effect on IL-8, one of the chemokines for eosinophils, released from eosinophils isolated from atopic diseases. [4] |
| In vivo | Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. [1] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (174.97 mM), Sonication is recommended.
H2O : 52 mg/mL (181.96 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (7 mM), Sonication is recommended.
Ethanol : 53 mg/mL (185.46 mM), Sonication is recommended.
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| Keywords | WAL-801 | WAL801 | WAL 801 | vertebrate | neuronal | mast | insect | Inhibitor | inhibit | HT | HistamineReceptor | Histamine Receptor | Epinastine Hydrochloride | Epinastine | cell | Antihistamine | antiallergic | 5HTReceptor | 5HT Receptor |
| Inhibitors Related | Kaolin | Alverine citrate | Rhamnose monohydrate | Meclizine dihydrochloride | D(+)-Raffinose pentahydrate | Famotidine | Hydroxypropyl Cellulose | 1,8-Cineole | Tributyrin | Sodium butanoate | Gluconate Calcium | Alginic acid |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
