| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Dopamine reuptake
The primary targets of Medifoxamine include the serotonin transporter (SERT) and dopamine transporter (DAT), as well as 5-HT2 and 5-HT1 receptors. It acts as a reuptake inhibitor for serotonin and dopamine, increasing their synaptic levels. Additionally, it has affinity for histamine H1 receptors and alpha-1 adrenergic receptors, contributing to its side effect profile. Its multi-receptor action is similar to some atypical antidepressants. |
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| ln Vitro |
In vitro, Medifoxamine inhibits serotonin and dopamine uptake in synaptosomal preparations with IC₅₀ values in the micromolar range. It also binds to 5-HT2 receptors with moderate affinity. In cell-based assays, it increases extracellular monoamine levels in neuronal cultures. These effects confirm its role as a reuptake inhibitor and receptor antagonist.
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| ln Vivo |
Medifoxamine is a novel monoamine re-uptake inhibiting antidepressive drug which preferentially inhibits dopamine reuptake. In human volunteer studies it has been found to reduce significantly intraocular pressure after single oral doses of 300-1000 mg, and to produce a small but statistically significant miosis. Its maximal ocular hypotensive action was less than that of oral timolol 20 mg[1].
In vivo, Medifoxamine has shown antidepressant-like activity in animal models, such as the forced swim test and the learned helplessness paradigm. It also exhibits anxiolytic effects. However, its clinical development was limited due to side effects and the emergence of newer antidepressants. It remains a tool for studying monoamine systems. |
| Enzyme Assay |
In vitro receptor binding studies for Medifoxamine measure its affinity for various receptors and transporters. Radioligand displacement assays using membrane preparations from rat brain or recombinant cells are performed. IC₅₀ values for SERT, DAT, and 5-HT2 receptors are determined. Selectivity over other targets is assessed.
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| Cell Assay |
In vitro cell-based assays for Medifoxamine evaluate its effects on neurotransmitter uptake. Neuronal cell lines such as SH-SY5Y are treated with the compound, and the uptake of radiolabeled serotonin or dopamine is measured. The compound's effect on intracellular calcium or cAMP signaling can also be studied to assess receptor antagonism.
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| Animal Protocol |
In vivo animal studies for Medifoxamine involve behavioral tests in rodents. The compound is administered orally or intraperitoneally. Antidepressant effects are assessed by forced swim test, tail suspension, and open field tests. Brain levels of monoamines are measured post-mortem to confirm target engagement.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Medifoxamine include good oral bioavailability and moderate half-life. It is metabolized in the liver. Its molecular weight is 325.40 g/mol. Storage is at room temperature. More detailed PK data are not widely available.
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| Toxicity/Toxicokinetics |
Oral LD50 in mice: 750 mg/kg. Sensory organs and special senses: pupillary dilation: eye; behavior: excitement; behavior: changes in motor activity (specific test). Therapie., 26(553), 1971 [PMID:5113808]
The toxicity profile of Medifoxamine includes typical antidepressant side effects such as dry mouth, drowsiness, and weight gain. It may also cause orthostatic hypotension. The compound is not approved for human use and is only available for research. |
| References |
[1]. Ocular hypotensive effects of medifoxamine. Br J Clin Pharmacol. 1992;34(3):269-271.
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| Additional Infomation |
Medifosamine is an aromatic ether. Medifosamine was marketed in France, Spain, and Morocco in the 1990s as an atypical antidepressant with anxiolytic effects, but was later withdrawn from the market due to cases of hepatotoxicity.
Additional information: Medifoxamine is also known as CGP-6085. It is a derivative of benzofuran. It was studied in clinical trials but never marketed. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C16H19NO2
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|---|---|
| Molecular Weight |
257.32756
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| Exact Mass |
257.142
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| CAS # |
32359-34-5
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| Related CAS # |
16604-45-8 (fumarate)
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| PubChem CID |
36109
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| Appearance |
White to off-white solid powder
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| Density |
1.076g/cm3
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| Boiling Point |
380ºC at 760mmHg
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| Flash Point |
132.9ºC
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| LogP |
3.032
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
19
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| Complexity |
213
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CC(OC1C=CC=CC=1)OC1C=CC=CC=1
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| InChi Key |
QNMGHBMGNRQPNL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19NO2/c1-17(2)13-16(18-14-9-5-3-6-10-14)19-15-11-7-4-8-12-15/h3-12,16H,13H2,1-2H3
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| Chemical Name |
N,N-dimethyl-2,2-diphenoxyethanamine
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| Synonyms |
Medifoxamine; 32359-34-5; N,N-Dimethyl-2,2-diphenoxyethanamine; Medifoxamina; Medifoxamine [INN:DCF]; (Dimethylamino)acetaldehyde diphenyl acetal; Medifoxaminum; Medifoxaminum [INN-Latin];
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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 |
| 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 (~388.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.72 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 (9.72 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 (9.72 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 | 3.8861 mL | 19.4303 mL | 38.8606 mL | |
| 5 mM | 0.7772 mL | 3.8861 mL | 7.7721 mL | |
| 10 mM | 0.3886 mL | 1.9430 mL | 3.8861 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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