Tesofensine is a triple monoamine reuptake inhibitor (DA, NA, 5-HT) originally developed for Parkinson’s and Alzheimer’s disease before its potent weight-reducing effects were observed in clinical trials. Inhibits presynaptic dopamine, noradrenaline, and serotonin transporters — raising synaptic monoamine concentrations in reward, appetite, and thermogenesis circuits. The uniquely long half-life (~9 days) means once-weekly dosing is theoretically achievable. Weight loss mechanism: appetite suppression via hypothalamic 5-HT/NA signalling + increased energy expenditure via sympathetic activation. Phase 2 RCT: 12.8% body weight reduction at 1mg/day over 24 weeks — among the highest seen outside GLP-1 receptor agonists.
Phase 2 RCT (Astrup et al. 2008 Lancet): tesofensine 0.25-1mg/day in obese patients over 24 weeks — dose-dependent weight loss 6.5-12.8%. Appetite suppression primary mechanism (EI diary, satiety scores). Higher efficacy than any approved monoamine-based anti-obesity drug.
Monoamine Transporter Pharmacology
Triple DAT/NAT/SERT inhibitor with distinct potency ratios vs other triple reuptake inhibitors. Reference compound for monoamine transporter selectivity assays, transporter occupancy studies, and neurochemical mapping.
Neurodegeneration Research (Original Indication)
Originally developed for dopaminergic enhancement in Parkinson’s and cognitive enhancement in Alzheimer’s. Catecholamine elevation in nigrostriatal pathway — studied in MPTP rodent models. Phase 2 trials in Parkinson’s showed motor improvement.
Metabolic Rate / Thermogenesis
Sympathomimetic component (NAT inhibition → elevated NA) increases thermogenesis via brown adipose tissue activation and lipolysis. Distinct from GLP-1 pathway weight loss — provides alternative mechanistic research model for anti-obesity drug development.
Key Research Data
Study
Key Findings
Astrup et al. 2008 Lancet
Phase 2 RCT N=203: tesofensine 0.25/0.5/1mg — 6.5/11.3/12.8% weight loss at 24 weeks, dose-dependent, well-tolerated except pulse rate increase at 1mg
Hayashi & Stahl 2010 Neuropsych
Tesofensine in Parkinson’s: UPDRS motor score improvement, dopaminergic enhancement data
Bjursell et al. 2017 Obesity
Long-term tesofensine in DIO mice: sustained weight loss, metabolic improvements at low dose
Specifications
Format
Oral — 0.5mg per unit
Purity
≥99% HPLC
Identity
MS confirmed
Storage
Room temperature, protect from moisture
Half-life
~220 hours — among the longest of any weight loss research compound
FAQ
What is Tesofensine (NS2330)?
Tesofensine (NS2330) is a Triple monoamine reuptake inhibitor (dopamine, noradrenaline, serotonin). Tesofensine is a triple monoamine reuptake inhibitor (DA, NA, 5-HT) originally developed for Parkinson’s and Alzheimer’s disease before its potent weight-reducing effects were observed in clinical trials. Inhibits presynaptic dopamine, noradrenaline, and serot…
What research applications does Tesofensine support?
Phase 2 RCT (Astrup et al. 2008 Lancet): tesofensine 0.25-1mg/day in obese patients over 24 weeks — dose-dependent weight loss 6.5-12.8%. Appetite suppression primary mechanism (EI diary, satiety scores). Higher efficacy than any approved monoamine-based anti-obesity drug….
How does Tesofensine compare to similar compounds?
Triple DAT/NAT/SERT inhibitor with distinct potency ratios vs other triple reuptake inhibitors. Reference compound for monoamine transporter selectivity assays, transporter occupancy studies, and neurochemical mapping….
Does QSC ship Tesofensine to the USA?
Yes. QSC ships domestically across the USA and to EU, UK, Canada, and Australia. Every batch carries a Janoshik third-party COA confirming ≥99% HPLC purity and MS identity.
