| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
The primary target of Pheniprazine hydrochloride is monoamine oxidase (MAO), specifically both MAO-A and MAO-B isoforms, though it is more potent as an MAO-A inhibitor. By irreversibly binding to the enzyme, it prevents the oxidative deamination of monoamine neurotransmitters, leading to elevated levels of serotonin, norepinephrine, and dopamine in the brain. This mechanism underlies its antidepressant and anxiolytic effects. It has been used in research to study the role of MAO in mood regulation.
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| ln Vitro |
In vitro, Pheniprazine hydrochloride is a potent inhibitor of MAO activity. Its inhibitory effect can be measured using enzyme assays that monitor the oxidation of substrates like kynuramine or benzylamine. The compound's irreversible nature is confirmed by the need for de novo enzyme synthesis to restore activity. Its IC₅₀ values for MAO-A and MAO-B are in the low micromolar range, though exact numbers may vary depending on the assay conditions.
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| ln Vivo |
In vivo, Pheniprazine hydrochloride has been shown to produce antidepressant-like effects in animal models of depression, such as the forced swim test and tail suspension test. It increases brain monoamine levels, which correlates with its behavioral effects. The compound has been studied in clinical settings for depression, but due to its potent and irreversible MAO inhibition, it has a significant side-effect profile and is now mainly a research tool.
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| Enzyme Assay |
In vitro enzyme assays for Pheniprazine hydrochloride measure the inhibition of MAO activity. The enzyme is typically prepared from rat brain mitochondria or recombinant human MAO-A and MAO-B. The compound is preincubated with the enzyme, then a substrate (e.g., kynuramine) is added, and the formation of a fluorescent product (4-hydroxyquinoline) is monitored over time. IC₅₀ values are calculated from inhibition curves. These assays are for research purposes.
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| Cell Assay |
In vitro cell-based assays for Pheniprazine hydrochloride evaluate its effects on neurotransmitter levels and cell viability. Neuronal cell lines such as SH-SY5Y or PC12 cells are treated with the compound, and intracellular levels of monoamines can be measured by HPLC. The compound's cytotoxicity is assessed using MTT or LDH assays. These studies help characterize its pharmacological and toxicological profile at the cellular level.
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| Animal Protocol |
In vivo animal studies for Pheniprazine hydrochloride typically involve rodents. The compound is administered intraperitoneally or orally, and behavioral tests are performed. For example, the forced swim test measures immobility time, which is reduced by antidepressants. Brain tissue is collected for monoamine analysis using HPLC. Liver and kidney function may be assessed due to potential hepatotoxicity. All procedures must comply with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Pheniprazine hydrochloride include rapid absorption and extensive distribution. It is metabolized in the liver, and its irreversible inhibition of MAO results in a long-lasting effect that extends beyond the compound's half-life. Its molecular weight is 184.67 g/mol. The compound is typically stored at room temperature in a dry place.
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| Toxicity/Toxicokinetics |
The toxicity profile of Pheniprazine hydrochloride is significant. As an irreversible MAOI, it can cause hypertensive crisis when combined with tyramine-containing foods or sympathomimetic drugs. Hepatotoxicity and central nervous system stimulation are also concerns. It is classified as a research compound and is not approved for human use in most countries. Standard safety precautions should be taken.
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| References | |
| Additional Infomation |
See also: Pheniprazine Hydrochloride (note moved to).
Additional information: Pheniprazine hydrochloride is also known as JB-516 and pheniprazine HCl. It has the CAS number 66-05-7. It is a hydrazine derivative. Its use is primarily in research to understand MAO function and the neurobiology of depression. It is not a first-line treatment and is considered obsolete clinically. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C9H15CLN2
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|---|---|
| Molecular Weight |
186.68
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| Exact Mass |
186.092
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| CAS # |
66-05-7
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| Related CAS # |
Pheniprazine;55-52-7
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| PubChem CID |
5284445
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| Appearance |
White to off-white solid powder
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| LogP |
2.974
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
12
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| Complexity |
97.7
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HXCTUSBYMZQLKB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H14N2.ClH/c1-8(11-10)7-9-5-3-2-4-6-9/h2-6,8,11H,7,10H2,1H31H
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| Chemical Name |
(1-phenylpropan-2-yl)hydrazine hydrochloride
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| Synonyms |
Pheniprazine hydrochloride CCRIS 1417 Pheniprazine HCl Phenylisopropylhydrazine hydrochloride NSC-17766 NSC17766NSC 17766
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~535.68 mM)
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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 | 5.3568 mL | 26.7838 mL | 53.5676 mL | |
| 5 mM | 1.0714 mL | 5.3568 mL | 10.7135 mL | |
| 10 mM | 0.5357 mL | 2.6784 mL | 5.3568 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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