A histamine H1 receptor antagonist
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Levocabastine is a potent and selective histamine H1 receptor antagonist with an IC50 value of 8.32 nM (Kis = 62.5, 23,500, and 1,937 nM for H1, H2, and H3, respectively) for inhibition of phosphoinositide turnover on human conjunctival epithelial cells. It has been used in clinical formulations in eye drops and nasal sprays for the treatment of allergic conjunctivitis and allergic rhinitis, respectively. Levocabastine also binds with high affinity to the rat neurotensin-2 receptor with an IC50 value of 10 nM.
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