| Bioactivity | 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]. |
| Target | Neurokinin 1 receptor |
| Invitro | 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]. Animal Model: |
| Name | Eprazinone dihydrochloride |
| CAS | 10402-53-6 |
| Formula | C24H34Cl2N2O2 |
| Molar Mass | 453.44 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. R S Thrall, et al. Eprazinone Alters Lung Lavage Lipid Levels and Transtracheal Ion Transport. Exp Lung Res. May-Jun 1992;18(3):409-20. [2]. Yvonne Krautscheid, et al. Pharmacophore Modeling, Virtual Screening, and in Vitro Testing Reveal Haloperidol, Eprazinone, and Fenbutrazate as Neurokinin Receptors Ligands. J Chem Inf Model. 2014 Jun 23;54(6):1747-57. |
Eprazinone dihydrochloride
CAS: 10402-53-6 F: C24H34Cl2N2O2 W: 453.44
Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties.
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