Catalog No.S4253 Synonyms: WAL-801CL HCl
Molecular Weight(MW): 285.77
Epinastine is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.
Purity & Quality Control
Choose Selective Histamine Receptor Inhibitors
|Description||Epinastine is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.|
Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum.  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.  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.  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. 
|In vivo||Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. |
|In vitro||DMSO||57 mg/mL (199.46 mM)|
|Water||57 mg/mL (199.46 mM)|
|Ethanol||57 mg/mL (199.46 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02251613||Completed||Allergic Conjunctivitis||Alcon Research||December 2013||Phase 4|
|NCT00564421||Completed||Seasonal Allergic Rhinitis||Merck Sharp & Dohme Corp.||December 18 2007||Phase 3|
|NCT00489398||Withdrawn||Allergic Conjunctivitis||Hom Milton M. OD FAAO|Merck Sharp & Dohme Corp.||July 2007||Phase 4|
|NCT00407927||Completed||Seasonal Allergic Rhinitis||Merck Sharp & Dohme Corp.||December 2006||Phase 2|
|NCT01382654||Completed||Allergic Rhinitis||Merck Sharp & Dohme Corp.||September 2006||Phase 2|
|NCT02260037||Completed||Healthy||Boehringer Ingelheim||August 2001||Phase 1|
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