| Size | Price | |
|---|---|---|
| 250mg | ||
| Other Sizes |
| 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. |
|---|---|
| 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. |
| Molecular Formula |
C17H22N4O.2[HCL]
|
|---|---|
| Molecular Weight |
371.30466
|
| Exact Mass |
298.179
|
| CAS # |
25953-17-7
|
| Related CAS # |
Minaprine;25905-77-5
|
| PubChem CID |
4199
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
531.2ºC at 760 mmHg
|
| Flash Point |
275.1ºC
|
| Vapour Pressure |
2.29E-11mmHg at 25°C
|
| LogP |
3.009
|
| 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
|
| 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
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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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