Bepotastine

Bepotastine is a clinically established antihistamine API used in the treatment of allergic conditions including allergic rhinitis, allergic conjunctivitis, and urticaria. As a selective H1 receptor antagonist, Bepotastine blocks the action of histamine at peripheral H1 receptors without significant CNS penetration, thereby avoiding the sedative side effects commonly associated with first‑generation antihistamines. Bepotastine is available in both oral and ophthalmic formulations, with the topical ophthalmic solution (Bepreve®) indicated for the treatment of ocular itching associated with allergic conjunctivitis. Bepotastine continues to be an important therapeutic option for patients suffering from allergic diseases, offering a favorable safety and efficacy profile.

 

Product Parameters

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Parameter	Specification
Product Name	Bepotastine
CAS Number	125602-71-3
Molecular Formula	C₂₁H₂₅ClN₂O₃
Molecular Weight	388.89 g/mol
Melting Point	56 – 58 °C
Boiling Point	546.8 ± 50.0 °C
Density	1.26 g/cm³
Storage Condition	−20 °C, under inert atmosphere

 

Bioactivity

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Bepotastine is a non-sedating, selective histamine 1 (H1) receptor antagonist.

 

In Vitro Study

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Bepotastine possesses additional anti-allergic activity including stabilization of mast cell function , inhibition of eosinophilic infiltration,inhibition of IL-5 production,and inhibition of leukotriene B4(LTB4) and LTD4 activity.

 

At concentrations of 10–100 micrometers, βpotastine significantly inhibits antigen-induced IL-5 production in human peripheral blood mononuclear cells (PBMCs), and this effect is enhanced when PBMCs are pre-incubated with Bepotastine.

 

Leukotriene B4 increased the Ca2+ concentration in cultured neutrophils, and this concentration was inhibited by beparastine ethanesulfonate (1–100 μM). Leukotriene B4 also elevated the Ca2+ concentration in cultured dorsal root ganglion neurons, which was similarly inhibited by beparastine besylate (100 μM).

 

In Vivo Studies

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Bepalastine (10 mg/kg) inhibits scratching induced by intradermal histamine injection (100 nmol per site), but is ineffective against serotonin stimulation (100 nmol per site).

 

Bepalastine (1–10 mg/kg, oral administration) exhibits dose-dependent inhibition of scratching induced by substance P (100 nmol per site) and leukotriene B4 (0.03 nmol per site; Chemicalbook). In vivo, bepalastine dose-dependently suppresses the acceleration of histamine-induced vascular permeability, and in guinea pig studies, it inhibits homologous passive skin anaphylactic shock.

 

In mouse pruritus models, oral administration of Bepotastine inhibited the frequency and duration of scratching behavior.

 

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