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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $30 | In Stock | In Stock | |
| 10 mg | $48 | In Stock | In Stock | |
| 25 mg | $96 | In Stock | In Stock | |
| 50 mg | $155 | In Stock | In Stock | |
| 100 mg | $228 | In Stock | In Stock | |
| 200 mg | $328 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $32 | In Stock | 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. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.81 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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