Bepotastine is a Selective and Orally Active Second-generation Histamine H1 receptor Antagonist

Atopic dermatitis is a chronically relapsing inflammatory skin disease. The characteristics of atopic dermatitis are eczema and even pruritus. The mechanism of itching evoked in atopic dermatitis is still not fully understood. However, there exists adjuvant therapy with topical agents.

Dermatitis spontaneously develops in housed NC/Nga mice and has many similarities to human atopic dermatitis. Besides, the characterization of atopic dermatitis contains dry, pruritic, lichenified skin lesions. What’s more, there even demonstrate dermal infiltration of lymphocytes, eosinophils, mast cells, and macrophages develop on the face, ears, neck, and back.

In this article, we will introduce a selective and orally active second-generation Histamine H1 receptor antagonist, Bepotastine.

Bepotastine can suppress the expression of nerve growth factor (NGF). As a result, in RPMCs, Bepotastine (10, 100, 1000 µM; preincubates for 120 min) decreases the release of histamine-induced by A23187 treatment. Additionally, it reaches a statistically significant reduced level at 1000 µM.

Besides, In Guinea pigs (6-week-old) experimental allergic conjunctivitis models, Bepotastine inhibits PAF-induced conjunctival eosinophil infiltration.

Furthermore, Bepotastine (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of TNF-induced conjunctival eosinophil infiltration.
Besides, Pruritus is the most severe problem in atopic dermatitis. In analysis to evaluate the effect of antihistamine on atopic dermatitis. Bepotastine (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and duration of 14.57 seconds.
Additionally, Bepotastine (10 mg/kg; p.o.; once) significantly suppresses serum LTB-4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash.

In conclusion, Bepotastine is one of the second-generation, nonsedating antihistamines. At the same time, it has the potential for allergic rhinitis, allergic conjunctivitis, and urticaria/pruritus research.

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