Antazoline (hydrochloride)

Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC₅₀ of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC₅₀ = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV^[1][2][3]. In Vitro:Antazoline hydrochloride (10-100 μmol/L, 72 h) exhibits dose-dependent inhibition of HBV DNA and no significant cytotoxicity in HepAD38 cells^[2].
Antazoline hydrochloride (100 μmol/L, 5 d) has inhibitory effect against HBV DNA (EC₅₀ = 2.91 μmol/L) in HepAD38 cells^[2].
Antazoline hydrochloride (0.123-30 μmol/L, 96 h) has a significant inhibitory effect on HBV DNA in Huh7 cells (EC₅₀ = 2.349 μmol/L)^[2]. In Vivo:Antazoline hydrochloride (10 mg/kg, i.v., single dose) is mainly eliminated by the kidney after administration in SD rats^[1].