| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Dopamine reuptake
Medifoxamine targets monoamine oxidase enzymes (MAO-A and MAO-B). By inhibiting MAO, it prevents the breakdown of monoamine neurotransmitters (serotonin, norepinephrine, dopamine), leading to increased levels of these neurotransmitters in the synaptic cleft. The compound may also inhibit the reuptake of serotonin and dopamine, contributing to its antidepressant effects. |
|---|---|
| ln Vitro |
In vitro, Medifoxamine fumarate shows inhibitory activity against MAO-A and MAO-B. It inhibits the deamination of monoamine substrates such as serotonin, tyramine, and dopamine. The compound may also inhibit serotonin and dopamine reuptake in synaptosomal preparations. Specific IC50 values for MAO inhibition are not detailed in available literature.
|
| 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 been studied for its antidepressant effects in animal models. It may produce antidepressant-like effects in the forced swim test and tail suspension test in rodents. The compound may also have anxiolytic effects. Clinical studies have been conducted for the treatment of depression, but detailed pharmacokinetic and efficacy data are limited. |
| Enzyme Assay |
MAO-A and MAO-B inhibition is assessed using enzyme activity assays. MAO enzymes (from rat brain mitochondria or recombinant sources) are incubated with a monoamine substrate (e.g., kynuramine for MAO-A, benzylamine for MAO-B) and varying concentrations of Medifoxamine fumarate. The reaction is stopped and the deaminated product is measured spectrophotometrically or fluorometrically. IC50 values are calculated from inhibition curves.
|
| Cell Assay |
For cellular assays, neuronal cell lines (e.g., SH-SY5Y or PC12 cells) are treated with Medifoxamine fumarate at varying concentrations (1-100 μM). MAO activity is measured in cell lysates using fluorometric or radiometric assays. Neurotransmitter levels (serotonin, dopamine, norepinephrine) in cell culture supernatants or cell lysates may be measured by HPLC-ECD or ELISA to assess the functional effects of MAO inhibition. Cell viability is assessed by MTT assay.
|
| Animal Protocol |
For in vivo efficacy, rodents (rats or mice) are administered Medifoxamine fumarate orally or intraperitoneally at doses of 1-50 mg/kg. The forced swim test and tail suspension test are performed to assess antidepressant-like effects. Locomotor activity is monitored to rule out stimulant effects. For pharmacokinetic studies, blood samples are collected at various time points and drug concentrations are measured by LC-MS/MS. MAO activity in brain tissue may be measured ex vivo.
|
| References |
[1]. Ocular hypotensive effects of medifoxamine. Br J Clin Pharmacol. 1992;34(3):269-271.
|
| Molecular Formula |
C20H22NO6
|
|---|---|
| Molecular Weight |
372.3923
|
| Exact Mass |
373.153
|
| CAS # |
16604-45-8
|
| Related CAS # |
32359-34-5 (Parent);110-17-8 (Parent)
|
| PubChem CID |
6450232
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
597.4ºC at 760 mmHg
|
| Flash Point |
315.1ºC
|
| Vapour Pressure |
4.04E-15mmHg at 25°C
|
| LogP |
2.743
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
27
|
| Complexity |
332
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)CC(OC1=CC=CC=C1)OC2=CC=CC=C2.C(=CC(=O)O)C(=O)O
|
| InChi Key |
CSQUJXBMSDQIKM-WLHGVMLRSA-N
|
| InChi Code |
InChI=1S/C16H19NO2.C4H4O4/c1-17(2)13-16(18-14-9-5-3-6-10-14)19-15-11-7-4-8-12-15;5-3(6)1-2-4(7)8/h3-12,16H,13H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
|
| Chemical Name |
(E)-but-2-enedioic acid;N,N-dimethyl-2,2-diphenoxyethanamine
|
| Synonyms |
Cledial; MEDIFOXAMINE FUMARATE; Geraxyl; 16604-45-8; UNII-OAG6T7TVU2; OAG6T7TVU2; LG 152; EINECS 240-657-2;
|
| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6854 mL | 13.4268 mL | 26.8536 mL | |
| 5 mM | 0.5371 mL | 2.6854 mL | 5.3707 mL | |
| 10 mM | 0.2685 mL | 1.3427 mL | 2.6854 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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