COMPOUND WIKI
← Back to Database
Metabolic/AdipolyticWADA Prohibited

Tesofensine

Synonyms: NS2330, NS-2330

Sequence: (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane

Critical Safety & Regulatory Notice

Tesofensine is classified as a regulated, unapproved, or research-only substance. Doping/Regulatory Status: Not FDA approved. Investigational status. Not prohibited by WADA.. Clinical safety profiles for human use are deficient or not approved.

History & Discovery Timeline

Tesofensine was originally developed by NeuroSearch in the early 2000s and later licensed to Saniona. It was initially investigated for the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's. What it is: Tesofensine is a monoamine reuptake inhibitor that indirectly functions like a peptide modulator. It is classified as an investigational metabolic and adipolytic compound with strong appetite-suppressive qualities. Proposed Mechanisms & Research Findings: It works by inhibiting the reuptake of dopamine, serotonin, and noradrenaline in the brain. This increases synaptic concentrations of these neurotransmitters, modulating hypothalamic feeding centers to decrease food intake and increase energy expenditure. Regulatory & Safety Status: It is not FDA approved and remains in clinical trial phases. Successful Phase II trials (TIPO-1) demonstrated significant weight loss, but it is still undergoing regulatory review. Sourcing gray-market forms carries substantial psychological and cardiovascular risks. Athletic & Anti-Doping Status: It is not currently on the WADA prohibited list, but it is monitored due to its stimulant-like activity on the central nervous system.

Understanding Tesofensine Key Facts

Primary Target System:CNS
Residue Count / Length:10 Amino Acids
Primary Action & Category:Monoamine Reuptake Inhibitor (Metabolic/Adipolytic)
Primary Receptors:Serotonin Transporter (SERT), Dopamine Transporter (DAT), Norepinephrine Transporter (NET)
Tesofensine mechanism diagram
Figure 1: Detailed molecular mechanism pathways of Tesofensine (click to enlarge).