1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. Eprazinone dihydrochloride

Eprazinone dihydrochloride 

Cat. No.: HY-B2078A
Handling Instructions

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.

For research use only. We do not sell to patients.

Eprazinone dihydrochloride Chemical Structure

Eprazinone dihydrochloride Chemical Structure

CAS No. : 10402-53-6

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Description

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].

Animal Model: Adult male pathogen free Fischer 344 inbred rats (200-250 g)[1]
Dosage: 50 mg/kg, 100 mg/kg, and 200 mg/kg
Administration: Oral gavage; daily; for 4 days
Result: At a dose of 200 mg/kg significantly increased total and individual (with the exception of phosphatidylinositol) phospholipid levels and decreased total neutral lipids.
Molecular Weight

453.44

Formula

C₂₄H₃₄Cl₂N₂O₂

CAS No.

10402-53-6

SMILES

O=C(C1=CC=CC=C1)C(C)CN2CCN(CC(OCC)C3=CC=CC=C3)CC2.Cl[H].Cl[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

EprazinoneNeurokinin ReceptorNK receptorPhospholipidpulmonaryarterialpO2chloridetransportmucolyticsecretolyticantispasmodicantitussiveNK1RInhibitorinhibitorinhibit

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Eprazinone dihydrochloride
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