| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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| Other Sizes |
| Targets |
The pharmacological action of Bromantane is complex and involves multiple neurotransmitter systems. Its primary action is characterized as dopamine-positive activity: it blocks synaptosomal dopamine uptake at 50 µM and antagonizes the effects of neuroleptics. Furthermore, it inhibits neuronal serotonin uptake (50 µM) and modulates its metabolism, while exhibiting a weaker direct effect on the noradrenergic system (only observed at high concentrations >500 µM). Other studies indicate GABAergic activity, enhancing GABA-ergic mediation.
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| ln Vitro |
Regarding the in vitro activity of Bromantane, existing research primarily focuses on neurotransmitter uptake inhibition assays. Experimental data show that 50 µM Bromantane effectively blocks synaptosomal uptake of dopamine and serotonin in rat brains. Unlike classical stimulants, its inhibitory effect on norepinephrine uptake is relatively weak, only manifesting at high concentrations (exceeding 500 µM), indicating a selective modulation of the monoamine neurotransmitter system.
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| ln Vivo |
In animal studies, Bromantane exhibits significant nootropic and psychostimulant activities. It activates simple and complex behavioral patterns in mice and produces EEG effects typical of psychostimulants. Regarding anti-fatigue effects, its efficacy shows a mathematical correlation with the drug concentration in the brain, suggesting a direct enhancement of work capacity. Notably, at low doses (1-5 mg/kg), it reduces serotonin content in the rat brain but is effective in antagonizing sedation and hypothermia induced by neuroleptics (e.g., chlorpromazine) at 5 mg/kg. Bromantane has also demonstrated positive effects on learning and memory processes in maze and conditioned reflex tests.
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| Enzyme Assay |
For the in vitro mechanistic study of Bromantane, synaptosomal uptake assays are typically used rather than purified enzyme systems. Standard protocol: 1. Prepare rat brain synaptosomes (usually from the striatum or dopamine-rich regions). 2. Incubate synaptosomes with radiolabeled neurotransmitters (e.g., [³H]-dopamine or [¹⁴C]-serotonin) and varying concentrations of Bromantane (typically ranging from 1 µM to 500 µM) in Krebs-Ringer buffer. 3. After a set period (usually 5-10 minutes), terminate the uptake reaction by rapid filtration or centrifugation. 4. Measure the radioactivity trapped inside the synaptosomes to calculate the IC₅₀ value. Data indicate that Bromantane (50 µM) significantly inhibits dopamine and serotonin uptake.
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| Cell Assay |
As a compound primarily acting on the central nervous system, cell-based assays for Bromantane often use neuronal cell lines (e.g., PC12 or SH-SY5Y). Procedure: 1. Seed neuronal cells in culture plates and culture to appropriate density. 2. Expose cells to gradient concentrations of Bromantane (typically 0.1-100 µM) for a defined period (e.g., 24-48 hours). 3. Assess cell viability using MTT or CCK-8 assays to evaluate cytotoxicity. 4. Detect changes in the expression of neurotransmitter-synthesizing enzymes (e.g., tyrosine hydroxylase) or synaptic proteins via Western Blot or immunofluorescence. To study protective effects, cells can be pre-treated with Bromantane before exposure to oxidative stress or neurotoxins.
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| Animal Protocol |
Common animal models for evaluating the activity of Bromantane include rats and mice. A typical protocol involves: 1. Randomly divide experimental animals into treatment and control groups. 2. Administer Bromantane via oral gavage or intraperitoneal injection (effective doses typically range from 1-50 mg/kg; note that the LD50 is extremely high at 8100 mg/kg, indicating a wide safety margin). 3. Conduct behavioral tests 30-60 minutes post-administration. Common tests include: Open Field test (locomotor activity), Forced Swim/Tail Suspension tests (antidepressant-like effects), Maze tests (learning and memory), and Rotarod test (motor coordination and fatigue resistance). 4. Euthanize animals after the experiments and collect brain tissue for bioanalysis to measure neurotransmitter levels or drug concentrations, establishing pharmacokinetic-pharmacodynamic correlation models.
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| ADME/Pharmacokinetics |
The pharmacokinetics of Bromantane are significantly correlated with its pharmacodynamics. Research indicates that Bromantane rapidly crosses the blood-brain barrier to enter the CNS, and its concentration dynamics in the brain show a mathematical correlation with behavioral effects (e.g., enhanced work capacity) and electrophysiological indices. This correlation reveals the quantitative relationship between “blood/brain drug concentration” and “pharmacological effect intensity,” though the nature of this relationship changes over time post-administration. Bromantane is generally considered a long-acting adaptogen, with anti-fatigue effects potentially persisting even after the drug is cleared from the bloodstream.
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| Toxicity/Toxicokinetics |
The safety profile of Bromantane is characterized by a very high therapeutic index in rodents. The median lethal dose (LD50) in mice (intraperitoneal injection) is as high as 8100 mg/kg, while therapeutic doses can be as low as a few milligrams per kilogram. According to Material Safety Data Sheets (MSDS) from major suppliers, Bromantane is classified as a non-hazardous substance or mixture. However, it is noteworthy that in a 2024 forensic toxicology case in North America, Bromantane was detected alongside novel benzodiazepines (e.g., bromazolam) and methamphetamine. Given its emerging potential for abuse as a new psychoactive substance, the long-term effects of non-medical use on cardiovascular and mental health warrant further monitoring.
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| References |
[1]. https://pubchem.ncbi.nlm.nih.gov/compound/4660557
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| Molecular Formula |
C16H20BRN
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|---|---|
| Molecular Weight |
306.24
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| Exact Mass |
305.0779
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| Elemental Analysis |
C, 62.75; H, 6.58; Br, 26.09; N, 4.57
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| CAS # |
87913-26-6
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| Appearance |
White to off-white solid powder
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| Density |
1.388±0.06 g/cm3
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| Boiling Point |
404.8±28.0 °C
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| Melting Point |
106-108°C
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| LogP |
5
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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 |
2
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| Heavy Atom Count |
18
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| Complexity |
280
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| SMILES |
C1C2CC3CC1CC(C2)C3NC4=CC=C(C=C4)Br
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| InChi Key |
LWJALJDRFBXHKX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H20BrN/c17-14-1-3-15(4-2-14)18-16-12-6-10-5-11(8-12)9-13(16)7-10/h1-4,10-13,16,18H,5-9H2
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| Chemical Name |
N-(4-bromophenyl)adamantan-2-amine
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| Synonyms |
Bromantane; 87913-26-6; Bromantan; bromontan; N1ILS53XWK;
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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) |
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
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| 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 | 3.2654 mL | 16.3271 mL | 32.6541 mL | |
| 5 mM | 0.6531 mL | 3.2654 mL | 6.5308 mL | |
| 10 mM | 0.3265 mL | 1.6327 mL | 3.2654 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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