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Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $30 | In Stock | |
| 10 mg | $48 | In Stock | |
| 25 mg | $96 | In Stock | |
| 50 mg | $155 | In Stock | |
| 100 mg | $228 | In Stock | |
| 200 mg | $328 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $32 | In Stock |
| Description | Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties. |
| Targets&IC50 | 5-HT2:25 nM(Ki), α1-adrenoceptor:77 nM(Ki) |
| In vitro | Niaprazine demonstrates a low affinity for the vesicular monoamine transporter as well as D2, α2, β, H1, and mAch receptors. Notably, the (+)stereoisomer of Niaprazine shows a significantly higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, whereas it is poorly recognized by 5-HT1A and 5-HT1B binding sites[2]. |
| In vivo | Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 minutes post-treatment but reduces them 3-8 hours after treatment. Niaprazine also temporarily depletes rat brain noradrenaline (NA) and dopamine (DA) levels[3]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3]. |
| Molecular Weight | 356.44 |
| Formula | C20H25FN4O |
| Cas No. | 27367-90-4 |
| Smiles | CC(CCN1CCN(CC1)c1ccc(F)cc1)NC(=O)c1cccnc1 |
| Relative Density. | 1.165 g/cm3 |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (280.55 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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