NS2330
Tesofensine is a novel triple monoamine reuptake inhibitor that primarily targets the neurotransmitters noradrenaline, serotonin, and dopamine. Researchers primarily study it for its potential effects on appetite regulation and weight management in individuals with obesity. Key findings from studies indicate that chronic administration of tesofensine enhances the expression of brain-derived neurotrophic factor (BDNF) and activity-regulated cytoskeleton protein (Arc) in the hippocampus, which may be linked to its antidepressant potential and neurogenic effects. Furthermore, tesofensine is currently undergoing Phase III clinical trials to evaluate its efficacy and safety as an anti-obesity therapy. As research continues, tesofensine represents a promising candidate in the evolving landscape of pharmacological interventions for obesity.
| Formula | C17H23Cl2NO |
| Molecular Weight | 328.3 g/mol |
| CAS Number | 195875-84-4 |
| PubChem CID | 11370864 |
Not applicable
Approximately 8-10 hours
Tesofensine exhibits a long half-life suitable for once-daily dosing.
Tesofensine is a triple monoamine reuptake inhibitor that enhances neurotransmission of norepinephrine, serotonin, and dopamine by blocking their reuptake transporters, primarily affecting the SERT (serotonin transporter), NET (norepinephrine transporter), and DAT (dopamine transporter). This action leads to increased levels of these monoamines in the synaptic cleft, which modulates appetite regulation and may influence neuroplasticity through pathways such as the BDNF signaling pathway and the activation of the Arc gene, promoting neurogenesis in the hippocampus. While its effects on appetite and weight loss are noted, the complete mechanism of action remains not fully understood.
777
Total Citations
4
Human/RCT
3.3
Avg. Influence
2025
Latest
The review highlighted that tesofensine is among emerging anti-obesity therapies currently under investigation, alongside other drugs that have shown varying efficacy and safety profiles.
The review indicated that tesofensine is a promising triple monoamine reuptake inhibitor in development for obesity, reflecting the urgent need for novel pharmacological treatments for this global health crisis.
Researchers observed that various pharmacological agents, including the monoamine re-uptake inhibitor tesofensine, are being developed to target appetite expression in obesity, although their effects on eating behavior remain inadequately characterized.
The review noted that tesofensine is a potent triple reuptake inhibitor currently in Phase III trials for obesity, highlighting its potential as a future pharmacotherapy.
The review concluded that tesofensine exemplifies a new treatment approach targeting multiple mechanisms of energy balance control, which may lead to more effective obesity therapies.
The study demonstrated that chronic treatment with tesofensine significantly increases brain derived neurotrophic factor and activity-regulated cytoskeleton protein mRNA levels in the rat hippocampus, indicating potential antidepressant effects.
Li Yue, et al. · Nature communications · 2025
Researchers studied a new class of antidepressants called triple reuptake inhibitors (TRIs), which target serotonin, norepinephrine, and dopamine levels. They found that different TRIs bind to a brain protein in unique ways, potentially leading to more effective treatments with fewer side effects for patients with depression.
Key findings
Perez Claudia I, et al. · PloS one · 2024
Researchers studied tesofensine, a new anti-obesity drug, and found that it promotes significant weight loss in obese rats by targeting specific neurons in the brain that control feeding behavior. The study suggests that tesofensine may be effective in preventing weight regain after dieting, making it a promising option for obesity treatment.
Key findings
George Melvin, et al. · Journal of cardiovascular pharmacology and therapeutics · 2014
Researchers reviewed new and emerging drug molecules aimed at combating obesity, a growing health crisis linked to serious heart conditions. They found several promising candidates in clinical trials, including drugs that target the gut and the brain, which may offer better safety and efficacy compared to existing treatments.
Key findings
Schoedel K A, et al. · Clinical pharmacology and therapeutics · 2010
Researchers studied the effects of tesofensine, a new drug being developed for obesity, in recreational stimulant users. They found that tesofensine did not produce significant effects compared to a placebo and had a lower potential for abuse than traditional stimulants like D-amphetamine.
Key findings
No comprehensive human trials assessing the long-term efficacy and safety of tesofensine for obesity management have been published. Additionally, the precise mechanisms by which tesofensine influences appetite regulation and its effects on eating behavior remain poorly characterized and require further investigation.
Solubility
Tesofensine is moderately soluble in water and highly soluble in DMSO.
Lyophilized
Stable for 2+ years at -20°C, 12 months at 4°C
Reconstituted
Use within 14 days when refrigerated at 4°C
Avoid
Avoid repeated freeze-thaw cycles, direct light
Solvent
Bacteriostatic water or sterile saline recommended
Safety information is derived from published research and may not reflect all known risks. This is not medical advice.
🇩🇪DE
Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.
🇺🇸US
Not approved by the FDA. Not scheduled by the DEA.
🇦🇺AU
Not approved by the TGA. Not scheduled.
🇬🇧UK
Not approved by the MHRA. Not a controlled substance.
Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.
Publications per Year
6 total| Vendor | Amount | Price | Price/mg | Link |
|---|---|---|---|---|
BESTUmbrella LabsUS | 15mg | $79.99 | $5.33/mg | |
Umbrella LabsUS | 1mg | $99.99 | $99.99/mg | |
Glacier AminosUS | 0.5mg | $114.99 | $229.98/mg | |
crownwellresearch.comUS | 0.5mg | $115.00 | $230.00/mg | |
Orbitrex PeptideUS | 0.5mg | $129.99 | $259.98/mg |
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This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer