Epinastine (hydrochloride)

Epinastine hydrochloride (WAL801 hydrochloride) is a selective and orally active histamine H1 receptor antagonist, CD96/PVR inhibitor and mast cell stabilizer. Epinastine hydrochloride has high affinity for neuronal octopamine receptors in locusts (K_i = 2 nM) and honeybees (K_i = 1.1 nM). Epinastine hydrochloride inhibits TARC, IL-8, and IL-4. Epinastine hydrochloride activates anti-colon cancer immunity and inhibits Substance P (HY-P0201)-induced scratching behavior and increased vascular permeability. Epinastine hydrochloride can be used in the research of allergic diseases^{[1][2][3][4][5][6][7][8]}. IC50 & Target:neuronal octopamine receptors in locusts (K_i = 2 nM) and honeybees (K_i = 1.1 nM) In Vitro:Epinastine (50-100 μM) hydrochloride inhibits histamine release from rat peritoneal mast cells induced by antigen-antibody reaction^[1].
Epinastine hydrochloride shows high affinity for neuronal octopamine receptors in locusts (K_i = 2 nM) and honeybees (K_i = 1.1 nM), specifically displaces [³H]NC-5Z binding to these receptors^[2].
Epinastine (1-25 μg/mL; 3-24 h) hydrochloride dose- and time-dependently suppresses constitutive and Calcium ionophore-induced IL-8 release from human eosinophils of atopic patients^[3].
Epinastine hydrochloride (1 μM; preincubation for 15 min, then incubation for 19 h) tends to inhibit PHA (HY-N7038)-induced IL-4 mRNA expression in peripheral blood mononuclear cells (PBMC) from asthmatic patients^[4].
Epinastine hydrochloride (0.1 μM - 10 μM; 24 h) inhibits IgE secretion from rat IgE-producing hybridoma FE-3 cells^[5].
In Vivo:Epinastine (1-30 mg/kg; p.o.; 60 min before stimulation) hydrochloride inhibits Substance P (HY-P0201)-induced scratching behavior and vascular permeability increase in ddY mice, but does not affect Dinitrofluorobenzene-induced scratching behavior in BALB/c mice^[7].
Epinastine (2-6 mg/kg; i.p.; 14 days) hydrochloride significantly inhibits tumor growth in C57BL/6N mice bearing MC38 tumors, enhances infiltration and IFN-γ secretion of CD8⁺ T cells and NK cells in tumor tissues, and has no toxicity to major organs^[8].