A histamine H1 receptor antagonist (Kiapps = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes

Epinastine (hydrochloride) – 100 mg

Brand:
Cayman
CAS:
108929-04-0
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Epinastine is a histamine H1 receptor antagonist (Kiapps = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer.{48871,48872} It inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human cord blood stem cell-derived mast cells (CBMCs) when used at a concentration of 0.1 μg/ml.{48872} Epinastine inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively).{11338} It inhibits dye leakage into the conjunctiva in a rat model of passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva (ID50 = 9.7 mg/kg, p.o.).{48873} Topical administration of formulations containing epinastine (0.05% three times per day) reduces lid edema, tearing, and redness, as well as the number of neutrophils and eosinophils in the lid fornix, in a mouse model of atopic conjunctivitis.{48872} Formulations containing epinastine have been used in the prevention of itching associated with allergic conjunctivitis.  

 

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Description

A histamine H1 receptor antagonist (Kiapps = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer; inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human CBMCs at 0.1 μg/ml; inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively); inhibits dye leakage into the conjunctiva in a rat model of passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva (ID50 = 9.7 mg/kg, p.o.); topical administration reduces lid edema, tearing, and redness, as well as the number of neutrophils and eosinophils in the lid fornix, in a mouse model of atopic conjunctivitis

Formal name: 9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepin-3-amine, monohydrochloride

Synonyms:  WAL 801CL

Molecular weight: 285.8

CAS: 108929-04-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases|Asthma||Research Area|Neuroscience|Ophthalmology

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