Quick Facts
- Category
- Weight Management
- Molecular Weight
- ~314 g/mol (free base)
- Half-Life
- ~9 days (~220 hours)
- CAS Number
- 195875-84-4
- Storage
- 15-25°C, dry, protected from light
- Solubility
- Sparingly soluble in water; soluble in DMSO and ethanol
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Description
Tesofensine (NS2330) is a small-molecule triple monoamine reuptake inhibitor originally developed by NeuroSearch for neurodegenerative research. Subsequent clinical investigations identified pronounced body-weight reductions in study participants, redirecting the compound into metabolic research. Unlike the GLP-1/GIP/glucagon agonist peptides, tesofensine is a non-peptide reference compound typically supplied as oral tablets for laboratory research.
Research Summary
The Phase II TIPO-1 trial (Astrup et al., The Lancet 2008) reported dose-dependent body-weight reductions in obese study participants over 24 weeks compared to placebo. Earlier Phase II programs investigating Parkinson's and Alzheimer's disease did not advance to late-stage development. A Phase III obesity programme was discontinued by the originator, while obesity research and selective regulatory approvals have continued in some jurisdictions through licensing partners.
Mechanism of Action
Tesofensine inhibits presynaptic reuptake of three monoamines, with the highest in-vitro affinity for the norepinephrine transporter (NET), followed by the dopamine transporter (DAT) and the serotonin transporter (SERT). The proposed basis for its appetite-suppressing and energy-expenditure effects observed in metabolic research is sustained enhancement of central monoaminergic tone, particularly noradrenergic and dopaminergic signalling in hypothalamic feeding circuits.
Known Research Compound Interactions
Based on published preclinical research literature
For laboratory research reference only. Not for human consumption. Interaction data derived from preclinical studies and receptor binding profiles. Always consult primary literature for specific research protocols.
Interaction assessments based on receptor binding affinity, signaling pathway analysis, and published preclinical data. For laboratory research use only. Not for human consumption.
For laboratory research use only. Not for human consumption.