| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Nomifensine Maleate acts as a potent inhibitor of dopamine (DA) and norepinephrine (NE) reuptake. It blocks the dopamine and norepinephrine transporters, increasing the synaptic availability of these neurotransmitters. This mechanism is responsible for its antidepressant effects. It is a selective inhibitor of dopamine uptake and was used in adult attention deficit disorder.
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| ln Vitro |
In vitro, nomifensine maleate is a potent inhibitor of dopamine and norepinephrine reuptake in rat brain synaptosomes. Its activity can be assessed using synaptosome preparations or cells expressing the dopamine or norepinephrine transporters. The inhibition of [³H]-dopamine or [³H]-norepinephrine uptake is measured in the presence of varying concentrations of the compound.
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| ln Vivo |
In vivo, nomifensine maleate was used as an antidepressant for the treatment of depression. It was later withdrawn from the market due to safety concerns. It remains an important compound in scientific research.
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| Enzyme Assay |
Non-cellular assays for nomifensine maleate are not standard, as it is a neurotransmitter reuptake inhibitor. Its binding affinity for the dopamine and norepinephrine transporters can be assessed using radioligand binding displacement studies with membrane preparations from cells expressing these transporters. The compound's inhibition of neurotransmitter uptake can be assessed in synaptosome preparations.
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| Cell Assay |
In vitro cellular assays for nomifensine maleate involve treating cells expressing the dopamine transporter (DAT) or norepinephrine transporter (NET) with the compound and measuring its effects on neurotransmitter uptake. Cells are incubated with [³H]-dopamine or [³H]-norepinephrine in the presence of varying concentrations of nomifensine maleate. The amount of radiolabeled neurotransmitter taken up into the cells is measured, and the IC₅₀ for inhibition of uptake is determined.
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| Animal Protocol |
In vivo animal experiments with nomifensine maleate are not typically conducted, as it is a withdrawn drug. Historical studies would have been conducted in animal models of depression to assess its antidepressant effects. The compound's effects on dopamine and norepinephrine levels in the brain would have been measured using microdialysis.
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| ADME/Pharmacokinetics |
Nomifensine Maleate has a molecular weight of 354.41 and a molecular formula of C₂₀H₂₂N₂O₄. It is a solid powder. The compound is soluble in DMSO and is typically stored at room temperature in a dry, dark place. It is stable under recommended storage conditions. Its CAS number is 32795-47-4.
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| Toxicity/Toxicokinetics |
Nomifensine Maleate is a research compound for laboratory use only and is not intended for human therapeutic or diagnostic use. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation. Appropriate personal protective equipment should be used.
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| References | |
| Additional Infomation |
An isoquinoline derivative that prevents dopamine reabsorption into the synaptosome. Maleate was once used to treat depression. Due to its potential to cause acute hemolytic anemia with intravascular hemolysis, it was withdrawn from the market globally in 1986. Kidney failure may also occur in some cases. (From Martindale Pharmacopoeia, 30th edition, p. 266)
See also: Nomifencin (note moved here). Nomifensine Maleate (CAS 32795-47-4) is a potent inhibitor of dopamine and norepinephrine reuptake. It was developed as an antidepressant in the 1970s but was withdrawn due to safety concerns. Nomifensine Maleate remains an important compound in scientific research and is available from various commercial suppliers for research applications. |
| Molecular Formula |
C20H22N2O4
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|---|---|
| Molecular Weight |
354.39968
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| Exact Mass |
354.158
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| Elemental Analysis |
C, 67.78; H, 6.26; N, 7.90; O, 18.06
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| CAS # |
32795-47-4
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| Related CAS # |
Nomifensine; 24526-64-5
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| PubChem CID |
5358907
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| Appearance |
Solid powder
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| Density |
1.114g/cm3
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| Boiling Point |
378.4ºC at 760mmHg
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| Melting Point |
179-181ºC
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| Flash Point |
164ºC
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| Index of Refraction |
1.581
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| LogP |
3.077
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
391
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1=CC=CC2=C1CN(C)CC2C3=CC=CC=C3.O=C(O)/C=C\C(O)=O
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| InChi Key |
GEOCVSMCLVIOEV-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C16H18N2.C4H4O4/c1-18-10-14(12-6-3-2-4-7-12)13-8-5-9-16(17)15(13)11-18;5-3(6)1-2-4(7)8/h2-9,14H,10-11,17H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;2-methyl-4-phenyl-3,4-dihydro-1H-isoquinolin-8-amine
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| Synonyms |
Nomifensine Maleate
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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: ≥ 80 mg/mL (~225.7 mM)
H2O: ~2.2 mg/mL (~6.2 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (7.76 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 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.75 mg/mL (7.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 27.5 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: ≥ 2.75 mg/mL (7.76 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 | 2.8217 mL | 14.1084 mL | 28.2167 mL | |
| 5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL | |
| 10 mM | 0.2822 mL | 1.4108 mL | 2.8217 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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