NS2330
Tesofensine is a novel triple monoamine reuptake inhibitor derived from the structure of a compound originally developed for Parkinson's disease. Researchers primarily study it for its potential effects on weight loss and its antidepressant properties. 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, suggesting a role in neurogenesis and mood regulation. Additionally, preclinical evidence suggests that tesofensine may effectively reduce body weight by acting on multiple neurotransmitter pathways involved in appetite regulation. Currently, tesofensine is undergoing clinical trials to further evaluate its efficacy and safety as a treatment 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 acts as a triple monoamine reuptake inhibitor, increasing the levels of norepinephrine, serotonin, and dopamine by blocking their respective transporters (NET, SERT, and DAT). This modulation enhances neurotransmission and is associated with increased expression of brain-derived neurotrophic factor (BDNF) and activity-regulated cytoskeleton protein (Arc) in the hippocampus, promoting neurogenesis and potentially contributing to its antidepressant effects. While the precise signaling pathways involved are not fully elucidated, the drug's impact on monoamine levels suggests involvement in pathways related to mood regulation and neuroplasticity.
766
Total Citations
4
Human/RCT
3.3
Avg. Influence
2025
Latest
The review highlighted that tesofensine is among several emerging anti-obesity drugs currently under investigation for their efficacy and safety in weight management.
The review emphasized that tesofensine is a promising triple monoamine reuptake inhibitor in development for obesity treatment amidst the urgent need for new therapies.
The review indicated that tesofensine is among several drugs under development aimed at modulating appetite expression in obesity, although effects on eating behavior remain poorly characterized.
The review noted that tesofensine is a potent triple reuptake inhibitor currently in Phase III trials for obesity, offering potential for long-term management of the condition.
The review concluded that tesofensine, targeting multiple mechanisms of energy balance control, may lead to more efficacious and better-tolerated obesity treatments in the near future.
The study demonstrated that chronic treatment with tesofensine increases BDNF and Arc mRNA expression and enhances neurogenesis in the hippocampus of rats.
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 long-term human trials assessing the safety and efficacy of tesofensine for obesity treatment have been published. Additionally, the specific mechanisms by which tesofensine influences energy balance and appetite regulation in humans remain unclear, necessitating further investigation into its pharmacological action and potential side effects over extended use.
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 | |
Orbitrex PeptideUS | 0.5mg | $99.99 | $199.98/mg | |
Bulk Peptide WholesaleUS | 0.5mg | $100.00 | $200.00/mg | |
Glacier AminosUS | 0.5mg | $114.99 | $229.98/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