| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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| 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.
Bromantane acts primarily by inhibiting the reuptake of both dopamine and serotonin in the brain, thereby increasing the synaptic availability of these neurotransmitters. It also modulates GABAergic neurotransmission, contributing to its anxiolytic properties. At very high doses, Bromantane exhibits anticholinergic effects. Unlike classical psychostimulants that act primarily through dopamine release or reuptake inhibition, Bromantane's combined effects on dopaminergic, serotonergic, and GABAergic systems provide a balanced profile of stimulation and anxiolysis. The compound does not appear to have significant affinity for classical stimulant targets such as the dopamine transporter (DAT) in the same manner as amphetamines. |
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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.
In vitro activity of Bromantane has been characterized through neurotransmitter uptake inhibition assays. The compound inhibits dopamine and serotonin reuptake in synaptosomal preparations with moderate potency, consistent with its mechanism of action. Receptor binding studies indicate that Bromantane has low to moderate affinity for various neurotransmitter receptors, including dopamine D2, serotonin 5-HT, and adrenergic receptors, though its primary effect is on reuptake inhibition rather than direct receptor agonism or antagonism. The compound's in vitro profile supports its classification as an atypical psychostimulant with a broader pharmacological spectrum than traditional stimulants. |
| 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.
In vivo, Bromantane demonstrates psychostimulant and anxiolytic effects in animal models. It enhances locomotor activity, improves performance in cognitive tasks, and reduces anxiety-like behaviors in rodent models. The compound increases physical endurance in forced swim tests and improves recovery from fatigue. Its effects on dopamine and serotonin neurotransmission in vivo have been confirmed through microdialysis studies showing increased extracellular levels of these neurotransmitters in brain regions such as the prefrontal cortex and striatum. Bromantane also shows neuroprotective properties in models of cerebral ischemia and oxidative stress, consistent with its actoprotector classification. |
| 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.
In vitro enzyme/receptor binding assays for Bromantane typically employ radioligand competition binding using membrane preparations from cells expressing dopamine, serotonin, or other neurotransmitter receptors. Synaptosomal uptake assays measure the compound's ability to inhibit [³H]-dopamine or [³H]-serotonin uptake into rat brain synaptosomes, providing IC50 values for reuptake inhibition. Receptor binding affinities (Ki) are determined by displacement of selective radioligands (e.g., [³H]-SCH23390 for D1, [³H]-spiperone for D2, [³H]-ketanserin for 5-HT2A). Selectivity profiling against a panel of 50-100 receptors, ion channels, and transporters helps characterize the compound's pharmacological spectrum. |
| 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.
In vitro cellular assays for Bromantane are performed in neuronal cell lines or primary neuronal cultures to assess its effects on neurotransmitter uptake, receptor signaling, and neuroprotection. Dopamine and serotonin uptake assays use cells expressing the respective transporters (DAT, SERT) or synaptosomal preparations. Signaling assays measure changes in intracellular cAMP (for GPCRs) or calcium flux following receptor activation. Neuroprotection assays evaluate the compound's ability to protect neurons from oxidative stress, glutamate excitotoxicity, or other insults. Cell viability is measured using MTT or LDH release assays. The compound's effects on neurite outgrowth and synaptic protein expression may also be assessed in differentiated neuronal cultures. |
| 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.
In vivo animal studies with Bromantane are conducted in rodent models to evaluate its psychostimulant, anxiolytic, and actoprotector properties. Typical behavioral assays include open field test (locomotor activity), elevated plus maze or light-dark box (anxiety), forced swim test or tail suspension test (depression-like behavior), and novel object recognition or Morris water maze (cognitive function). Physical endurance is assessed using forced swim or treadmill running tests. Neurochemical studies measure neurotransmitter levels in brain tissue or microdialysate by HPLC-ECD. Neuroprotective effects are evaluated in models of cerebral ischemia, traumatic brain injury, or neurodegenerative disease. Dosing is typically via intraperitoneal or oral administration. |
| 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.
Pharmacokinetic properties of Bromantane have been characterized in preclinical and clinical studies. Following oral administration, the compound is rapidly absorbed with Tmax of 1-2 hours and a plasma half-life of approximately 10-12 hours. Bromantane is extensively metabolized in the liver via cytochrome P450-mediated oxidation, with metabolites excreted in urine. The compound exhibits high oral bioavailability and good blood-brain barrier permeability, consistent with its CNS activity. Protein binding is moderate, and tissue distribution shows accumulation in brain, liver, and kidney. Pharmacokinetic parameters may vary between species and formulations. |
| 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.
Toxicological evaluation of Bromantane has been conducted as part of its clinical development in Russia. The compound is generally well-tolerated at therapeutic doses, with a favorable safety profile compared to classical psychostimulants. Preclinical toxicology studies have assessed acute and repeat-dose toxicity, genotoxicity, and reproductive toxicity. Common adverse effects reported in clinical use include mild insomnia, headache, and gastrointestinal discomfort. No significant cardiotoxicity or abuse potential has been reported. The compound is not recommended for use in patients with severe renal impairment. Long-term safety data are available from its clinical use in Russia. |
| References |
[1]. https://pubchem.ncbi.nlm.nih.gov/compound/4660557
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| Additional Infomation |
Bromantane (Ladasten) is a synthetic actoprotector and psychostimulant developed in Russia and used clinically for neurasthenia and performance enhancement. Its mechanism involves inhibition of dopamine and serotonin reuptake, combined with GABAergic modulation. It is approved for medical use in Russia but not by the FDA or EMA. The compound shows potential as a cognitive enhancer, fatigue fighter, and anxiolytic. Research continues into its neuroprotective properties and applications in chronic fatigue and neurodegenerative conditions.
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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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| PubChem CID |
4660557
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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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| Defined Atom Stereocenter Count |
0
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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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