| Size | Price | Stock | Qty |
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| 1mg | |||
| 5mg | |||
| 10mg | |||
| 50mg |
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| Other Sizes |
| Targets |
The primary target of Piribedil N-oxide is the alpha2-adrenergic receptor, where it acts as an antagonist. It is a metabolite of the dopamine receptor agonist piribedil, which itself targets dopamine D2 and D3 receptors. However, the N-oxide metabolite does not necessarily retain the dopaminergic activity of the parent drug. The compound is classified as a drug metabolite and is used to study the metabolic fate of piribedil.
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| ln Vitro |
Piribedil N-oxide has been found to be an alpha2-adrenergic antagonist, which suggests it may have activity opposite to that of the parent drug piribedil (a dopamine D2/D3 agonist) in certain biological systems. It is a metabolite of the dopamine receptor agonist piribedil, representing a chemical compound involved in the metabolic processing of its parent compound. The compound could be used to improve cognition and sensory neurological disorders, indicating potential neuropharmacological activity.
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| ln Vivo |
No specific in vivo data was found for Piribedil N-oxide as an administered drug. Its description as a compound that could be used to improve cognition and sensory neurological disorders suggests potential therapeutic utility, but specific in vivo studies and efficacy data are not provided in the summarized literature. It is primarily used as an analytical standard for studying the metabolism of piribedil rather than as a drug candidate.
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| Enzyme Assay |
Standard alpha2-adrenergic receptor binding assay: Membrane preparations from rat brain cortex or cells expressing human alpha2A/2B/2C-adrenoceptors are incubated with 0.5-1 nM [3H]-RX821002 or [3H]-rauwolscine and varying concentrations of Piribedil N-oxide (0.1-10,000 nM) in 50 mM Tris-HCl buffer (pH 7.4) at 25degC for 60 minutes. Non-specific binding is determined using 10 uM phentolamine. Bound radioactivity is separated by filtration through GF/B filters and quantified by scintillation counting. Ki values are calculated.
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| Cell Assay |
No specific cell-based protocols were found. For functional alpha2-adrenergic antagonist activity, cells expressing alpha2-adrenoceptors (e.g., CHO cells) are seeded in 96-well plates and pre-incubated with a forskolin-containing buffer to raise cAMP levels. alpha2-adrenoceptor activation by an agonist (e.g., clonidine) inhibits forskolin-stimulated cAMP accumulation. Test compounds are added to determine the concentration required to reverse this inhibition. Intracellular cAMP levels are measured by HTRF or ELISA.
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| Animal Protocol |
No specific in vivo animal protocols were found. A general protocol for studying a cognitive-enhancing compound: Rats are trained in the Morris water maze or passive avoidance task to establish baseline learning and memory. Piribedil N-oxide is administered orally or intraperitoneally at doses of 1-30 mg/kg, 30-60 minutes before testing. Performance parameters (escape latency in water maze, step-through latency in passive avoidance) are recorded. Cognitive function in treated animals is compared to control and positive control groups.
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| ADME/Pharmacokinetics |
No specific PK data was found for Piribedil N-oxide. As a metabolite of the parent drug piribedil, its formation from piribedil would be studied. Following oral administration of piribedil, plasma and tissue samples are collected and analyzed by LC-MS/MS to measure both the parent drug and its N-oxide metabolite. The rate of formation, Cmax, and exposure (AUC) of Piribedil N-oxide can be determined from these studies.
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| Toxicity/Toxicokinetics |
Piribedil N-oxide is a metabolite of the dopamine receptor agonist piribedil. The safety profile of the parent drug is better established: piribedil may cause gastrointestinal disturbances (nausea, vomiting), dizziness, drowsiness, hypotension, and psychiatric effects. As a metabolite, it may contribute to the overall activity or side effect profile of the parent drug. For research use only.
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| References | |
| Additional Infomation |
Piribedil N-oxide is a research-grade metabolite with molecular formula C16H18N4O3 and molecular weight 314.34. Purity >95%. It is the N-oxide metabolite of the dopamine receptor agonist piribedil and an alpha2-adrenergic antagonist. This product is intended for research use only, not for human therapeutic applications, and is supplied as an analytical standard for drug metabolism studies.
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| Molecular Formula |
C16H18N4O3
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|---|---|
| Molecular Weight |
314.34
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| Exact Mass |
314.138
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| CAS # |
53954-71-5
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| PubChem CID |
71441787
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| Appearance |
Typically exists as solids at room temperature
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| LogP |
1.564
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
397
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C[N+](CCN1C2=NC=CC=N2)(CC3=CC4=C(C=C3)OCO4)[O-]
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| InChi Key |
UOCNNJVJUXZOHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H18N4O3/c21-20(11-13-2-3-14-15(10-13)23-12-22-14)8-6-19(7-9-20)16-17-4-1-5-18-16/h1-5,10H,6-9,11-12H2
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| Chemical Name |
2-[4-(1,3-benzodioxol-5-ylmethyl)-4-oxidopiperazin-4-ium-1-yl]pyrimidine
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| Synonyms |
Piribedil N-oxide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1813 mL | 15.9063 mL | 31.8127 mL | |
| 5 mM | 0.6363 mL | 3.1813 mL | 6.3625 mL | |
| 10 mM | 0.3181 mL | 1.5906 mL | 3.1813 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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