Eprazinone (dihydrochloride)

Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen^[1][2]. IC50 & Target: Neurokinin 1 receptor^[1] In Vitro: Eprazinone specifically displaces binding to the NK1R. Although Eprazinone displays a rather weak inhibition of [¹²⁵I]BH-SP binding to NK1R, at a concentration of 25 μM, and an antagonistic effect of about 30%, NK1R blockade could contribute to its mucolytic activity^[2]. In Vivo: Eprazinone (50-200 mg/kg; oral gavage; daily; for 4 days; adult male rats) at a dose of 200 mg/kg significantly increases total and individual (with the exception of phosphatidylinositol) phospholipid levels and decreases total neutral lipids. Lower doses of Eprazinone significantly decrease neutral lipid levels without affecting the phospholipids^[1].
In airway epithelial studies, mucosal addition of Eprazinone produces a dose-dependent partially reversible decrease in short-circuit current (Isc). The decrease in Isc at lower Eprazinone concentrations is accounted for entirely by a decrease in net chloride secretion while at higher concentrations both sodium and chloride transport are affected^[1].