Epinastine HCl

Catalog No.S4253 Synonyms: WAL-801CL HCl

Epinastine HCl Chemical Structure

Molecular Weight(MW): 285.77

Epinastine is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.

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Biological Activity

Description Epinastine is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.
Targets
Histamine receptor [1]
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]

Protocol

Solubility (25°C)

In vitro DMSO 57 mg/mL (199.46 mM)
Water 57 mg/mL (199.46 mM)
Ethanol 57 mg/mL (199.46 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 285.77
Formula

C16H15N3.HCl

CAS No. 108929-04-0
Storage powder
Synonyms WAL-801CL HCl

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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
NCT01569191 Completed Ocular Allergy Aston University|University of Worcester March 2012 Phase 4
NCT00564421 Completed Seasonal Allergic Rhinitis Merck Sharp & Dohme Corp. December 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

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