| Size | Price | |
|---|---|---|
| 250mg | ||
| Other Sizes |
| Targets |
The primary targets of Minaprine include MAO-A, dopamine receptors, and serotonin receptors. It inhibits MAO-A reversibly, leading to increased levels of serotonin and norepinephrine. Additionally, it has weak affinity for D2 and 5-HT2 receptors, and it may act as an antagonist at these sites. Its mechanism is complex and may involve multiple neurotransmitter systems, contributing to its antidepressant and cognitive-enhancing effects.
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|---|---|
| ln Vitro |
In vitro, Minaprine inhibits MAO-A with an IC₅₀ in the low micromolar range. It also shows binding affinity for dopamine D2 and serotonin 5-HT2 receptors. In cell-based assays, it increases the release of neurotransmitters from synaptosomes. Its effects are more pronounced in the hippocampus and cortex. These activities confirm its role as a multi-target antidepressant.
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| ln Vivo |
In vivo, Minaprine has demonstrated antidepressant-like activity in animal models such as the forced swim test and learned helplessness. It improves cognitive performance in aged rats and reverses scopolamine-induced memory deficits. In human clinical studies, it was effective in treating depression with fewer sedative side effects compared to tricyclic antidepressants. However, its use was limited by hepatotoxicity.
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| Enzyme Assay |
In vitro enzyme assays for Minaprine measure its inhibition of MAO-A and MAO-B activity. The compound is incubated with human or rat brain mitochondria, and the oxidation of a substrate (e.g., serotonin or benzylamine) is monitored. IC₅₀ values are determined. Receptor binding assays using radioligands (e.g., [³H]spiperone for D2) assess its affinity for various neurotransmitter receptors.
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| Cell Assay |
In vitro cell-based assays for Minaprine evaluate its effects on neurotransmitter uptake and release. Neuronal cell lines are treated with the compound, and extracellular levels of serotonin, dopamine, and norepinephrine are measured by HPLC. Cell viability is assessed to rule out cytotoxic effects. These assays help characterize its synaptic effects.
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| Animal Protocol |
In vivo animal studies for Minaprine involve behavioral testing in rodents. The compound is administered orally or intraperitoneally. The forced swim test and tail suspension test are used to assess antidepressant effects. Cognitive tests such as the Morris water maze are used for memory effects. Biochemical analyses of brain monoamine levels are performed post-mortem.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
The liver. Cytochrome P450 2D is responsible for the 4-hydroxylation of mirtazapine, producing 4-hydroxymirtazapine. Known human metabolites of mirtazapine include 4-hydroxymirtazapine. The pharmacokinetic properties of Minaprine include rapid absorption and extensive metabolism. It has a half-life of about 2-4 hours. It is metabolized by the liver, primarily via oxidation and glucuronidation. Its molecular weight is 356.29 g/mol. The compound should be stored at room temperature, protected from light. |
| Toxicity/Toxicokinetics |
The toxicity profile of Minaprine includes hepatotoxicity, which led to its withdrawal from the market. It can also cause agranulocytosis in rare cases. Other side effects include nausea, dizziness, and anxiety. It is not recommended for human use and is only available as a research chemical.
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| References | |
| Additional Infomation |
Minaprine belongs to the pyridazine, secondary amine, and morpholine classes of compounds. It has multiple effects, including antidepressant, serotonin reuptake inhibitor, dopamine reuptake inhibitor, cholinergic, and anti-Parkinson's disease drug. Minaprine is a psychotropic drug that has been proven effective in treating various depressive symptoms. Like most antidepressants, Minaprine antagonizes behavioral hopelessness. Minaprine is an aminophenylpyridazine antidepressant, and its incidence of cardiotoxicity, drowsiness, and weight gain has been reported to be relatively low. Drug Indications: For the treatment of depression. Mechanism of Action: Minaprine binds to serotonin type 2 receptors and dopamine D1 and D2 receptors. It also binds to the serotonin reuptake pump. Therefore, Minaprine blocks the reuptake of dopamine and serotonin. It also has mild cholinergic agonist effects. Therefore, it may simultaneously have mood-enhancing and brain-development-promoting effects. It also functions as a reversible inhibitor of monoamine oxidase A (MAO-A) (RIMA). Furthermore, it has been found to inhibit acetylcholinesterase.
Pharmacodynamics Minaprilin is an aminophenylpyridazine antidepressant with reportedly relatively low rates of cardiotoxicity, drowsiness, and weight gain. Similar to other antidepressants, mirtazaprilin attenuates the function of β-adrenergic receptors. Studies have also shown that mirtazaprilin improves memory consolidation, and repeated administration enhances this effect. Furthermore, mirtazaprilin's effect on memory consolidation is related to its dopaminergic activity. Additional information: Minaprine dihydrochloride was marketed under the brand name Cantor. It was used primarily in France. It is a pyridazine derivative with a unique dual action on MAO and receptors. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C17H22N4O.2[HCL]
|
|---|---|
| Molecular Weight |
371.30466
|
| Exact Mass |
298.179
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| CAS # |
25953-17-7
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| Related CAS # |
Minaprine;25905-77-5
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| PubChem CID |
4199
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| Appearance |
White to off-white solid powder
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| Boiling Point |
531.2ºC at 760 mmHg
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| Flash Point |
275.1ºC
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| Vapour Pressure |
2.29E-11mmHg at 25°C
|
| LogP |
3.009
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
22
|
| Complexity |
316
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LDMWSLGGVTVJPG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H22N4O/c1-14-13-16(15-5-3-2-4-6-15)19-20-17(14)18-7-8-21-9-11-22-12-10-21/h2-6,13H,7-12H2,1H3,(H,18,20)
|
| Chemical Name |
4-methyl-N-(2-morpholin-4-ylethyl)-6-phenylpyridazin-3-amine
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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) |
H2O : ~100 mg/mL (~269.32 mM)
DMSO : ≥ 100 mg/mL (~269.32 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 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 25.0 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: ≥ 2.5 mg/mL (6.73 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 25.0 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: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (269.32 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6932 mL | 13.4662 mL | 26.9324 mL | |
| 5 mM | 0.5386 mL | 2.6932 mL | 5.3865 mL | |
| 10 mM | 0.2693 mL | 1.3466 mL | 2.6932 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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