| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Niaprazine targets the histamine H1 receptor as an antagonist. It also has affinity for α1-adrenoceptors (Ki = 77 nM) and 5-HT2 receptors (Ki = 25 nM).
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| ln Vitro |
Niaprazine has minimal affinity for D2, α2, β, H1, and mAch receptors as well as the vesicular monoamine transporter. 5-HT1A and 5-HT1B binding sites do not recognize niaprazine well, while α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites do[2]. Niaprazine, in particular, the (+)stereoisomer, has a higher affinity for these sites.
Niaprazine is a histamine H1 receptor antagonist with antihistamine and antiserotonin activities. It exhibits a higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, particularly the (+)stereoisomer. It has low affinity for D2, α2, β, H1, and mAch receptors. |
| ln Vivo |
Rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations rise 30 minutes after niaprazine (60 mg/kg; ip; once) administration and fall 3–8 hours later. Moreover, niaprazine causes a transient reduction in dopamine (DA) and noradrenaline (NA) in rat brains[3].
In vivo, niaprazine (60 mg/kg; intraperitoneal injection) increases rat brain 5-HIAA concentrations 30 minutes after treatment, and reduces them at 3-8 hours after treatment. It also produces a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA). The compound exhibits significant sedative properties. |
| Enzyme Assay |
In vitro receptor binding assays for niaprazine are performed to evaluate its affinity for H1, α1, 5-HT2, and other receptors. Radioligand binding studies using membrane preparations from cells or tissues expressing the target receptors are conducted. The compound's ability to displace specific radiolabeled ligands is measured to calculate its Ki values.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing the target receptors. The cells are treated with niaprazine, and receptor activation or inhibition is measured by assessing downstream signaling events. The compound's antagonist activity at H1 receptors and its effects on serotonergic and adrenergic signaling are characterized.
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (150-200 g)[3]
Doses: 60 mg/kg Route of Administration: intraperitoneal (ip) injection; once Experimental Results: Increased rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and decreased them at 3-8 hr after treatment. In vivo animal studies are conducted in rodent models to evaluate the effects of niaprazine on sleep and neurotransmitter levels. The compound is typically administered via intraperitoneal injection at a dose of 60 mg/kg. Its effects on brain 5-HIAA, noradrenaline, and dopamine levels are assessed. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for niaprazine. As an orally active compound with sedative properties, its ADME properties would be characterized in standard preclinical studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for niaprazine. As an H1 receptor antagonist, its toxicity profile is expected to be related to its mechanism of action. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
Niapridine is a type of piperazine drug. Niapridine is a selective catecholamine depletor.
Niaprazine is a histamine H1 receptor antagonist with antihistamine and antiserotonin activities and significant sedative properties. It is used for sleep disorder research. The compound is not approved for human therapeutic use and is strictly for research purposes. |
| Molecular Formula |
C20H25FN4O
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|---|---|
| Molecular Weight |
356.44
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| Exact Mass |
356.201
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| CAS # |
27367-90-4
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| Related CAS # |
34426-53-4 (tri-hydrochloride)
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| PubChem CID |
71919
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| Appearance |
White to off-white solid powder
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| LogP |
3.129
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
434
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CCN1CCN(CC1)C2=CC=C(C=C2)F)NC(=O)C3=CN=CC=C3
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| InChi Key |
RSKQGBFMNPDPLR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25FN4O/c1-16(23-20(26)17-3-2-9-22-15-17)8-10-24-11-13-25(14-12-24)19-6-4-18(21)5-7-19/h2-7,9,15-16H,8,10-14H2,1H3,(H,23,26)
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| Chemical Name |
N-[4-[4-(4-fluorophenyl)piperazin-1-yl]butan-2-yl]pyridine-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (280.55 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.83 mg/mL (2.33 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (2.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8055 mL | 14.0276 mL | 28.0552 mL | |
| 5 mM | 0.5611 mL | 2.8055 mL | 5.6110 mL | |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8055 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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