| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Serotonin transporter (SERT); norepinephrine transporter (NET); dopamine D1/D2 receptors.
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| ln Vitro |
Melitracen inhibits the uptake of norepinephrine and serotonin (5-HT) through the presynaptic membrane, inducing an increase in monoamine transmitters in the synaptic space. It is a potential dopamine D1/2 receptor antagonist. The compound has antidepressant, anti-anxiety, and muscle relaxant effects. It is often co-administered with flupenthixol for trigeminal neuralgia.
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| ln Vivo |
In mice, an oral dose of imipramine or melitracen resulted in a notable and durable mydriasis. The mydriatic action of melitracen is more pronounced and persistent. Melitracene works better to arouse conduct. Melitracen, when taken orally, lowers catecholamine levels in the adrenal glands, spleen, brainstem, and cerebral cortex [2]. Rats given melitracen daily for 13 or 15 weeks showed no discernible changes in catecholamine levels in the brainstem, cerebral cortex, or spleen. Nonetheless, the adrenal glands' quantities of adrenaline somewhat drop [2].
Melitracen exerts antidepressant and anti-anxiety effects in vivo. It likely exerts its efficacy similarly to imipramine and amitriptyline by inhibiting serotonin-norepinephrine reuptake. The compound is orally active. It is used clinically for the treatment of depression and anxiety disorders, often in combination with flupenthixol. |
| Enzyme Assay |
In vitro receptor binding assays measure the affinity of Melitracen for serotonin and norepinephrine transporters. Membrane preparations from cells expressing recombinant human SERT or NET are incubated with radiolabeled ligands (e.g., [3H]imipramine or [3H]nisoxetine) and varying concentrations of Melitracen (typically 0.1 nM to 100 µM). Ki values are calculated from competition binding curves. Dopamine D1/D2 receptor binding is assessed using appropriate radioligands.
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| Cell Assay |
In vitro cellular assays are performed using neuronal cell lines or synaptosomal preparations. Cells are treated with Melitracen at concentrations ranging from 0.01-100 µM. Neurotransmitter uptake is measured using radiolabeled serotonin, norepinephrine, or dopamine. Intracellular cAMP levels are measured to assess dopamine receptor antagonism. Cell viability is monitored using MTT assays. Neurite outgrowth and neuronal differentiation can be assessed in appropriate cell models.
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| Animal Protocol |
In vivo efficacy is evaluated in rodent models of depression (e.g., forced swim test, tail suspension test) and anxiety (e.g., elevated plus maze). Melitracen is administered orally or intraperitoneally at doses ranging from 1-20 mg/kg. Behavioral parameters are scored. For trigeminal neuralgia studies, appropriate pain models are used. Neurotransmitter levels in brain tissue are measured by HPLC. The compound's effects on monoamine turnover are assessed.
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| ADME/Pharmacokinetics |
Melitracen hydrochloride has a molecular weight of 331.88 g/mol and molecular formula C20H23N·HCl. CAS number: 10563-70-9. It is orally active. Purity ≥98% by HPLC. Store as a powder at room temperature. Soluble in water and DMSO. For in vivo use, formulate in saline or suitable vehicle. The compound is stable under normal storage conditions.
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| Toxicity/Toxicokinetics |
Melitracen is generally well-tolerated at therapeutic doses. Side effects may include anticholinergic effects (dry mouth, constipation, urinary retention), drowsiness, and weight gain. As a tricyclic antidepressant, it may cause cardiac conduction abnormalities at high doses. Contraindications include recent myocardial infarction, arrhythmias, and glaucoma. The compound is for research use only.
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| References |
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| Additional Infomation |
Melitracen hydrochloride belongs to the anthracene class of compounds.
Melitracen hydrochloride is a tricyclic antidepressant used clinically for depression and anxiety. It is often co-administered with flupenthixol (as Flupenthixol/Melitracen combination) for the treatment of trigeminal neuralgia. The compound is also known as Thymeol. It is supplied as a research compound with high purity and should be stored at room temperature. |
| Molecular Formula |
C21H26CLN
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|---|---|
| Molecular Weight |
327.89
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| Exact Mass |
327.175
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| CAS # |
10563-70-9
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| Related CAS # |
Melitracen-d6 hydrochloride;1189648-08-5;Melitracen;5118-29-6
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| PubChem CID |
25381
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| Appearance |
White to off-white solid powder
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| Density |
1.046 g/cm3
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| Boiling Point |
399.1ºC at 760 mmHg
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| Melting Point |
245-248ºC
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| Flash Point |
174.4ºC
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| Vapour Pressure |
1.4E-06mmHg at 25°C
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| Index of Refraction |
1.607
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| LogP |
5.511
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
378
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RADLXCPDUXFGFF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25N.ClH/c1-21(2)19-13-7-5-10-17(19)16(12-9-15-22(3)4)18-11-6-8-14-20(18)21;/h5-8,10-14H,9,15H2,1-4H3;1H
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| Chemical Name |
3-(10,10-dimethylanthracen-9-ylidene)-N,N-dimethylpropan-1-amine;hydrochloride
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| Synonyms |
N-7001; N7001; N 7001
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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 (~304.98 mM)
DMSO : ~100 mg/mL (~304.98 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.62 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 (7.62 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 (7.62 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 | 3.0498 mL | 15.2490 mL | 30.4980 mL | |
| 5 mM | 0.6100 mL | 3.0498 mL | 6.0996 mL | |
| 10 mM | 0.3050 mL | 1.5249 mL | 3.0498 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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