Description
Tesofensine
NS-2330 · Oral Research Solution
A centrally-acting small molecule that inhibits the reuptake of dopamine, norepinephrine, and serotonin at once — a triple monoamine mechanism studied extensively in metabolic and appetite-regulation research. Supplied as a pre-mixed 30 mL solution at 0.5 mg/mL.
One molecule acting on all three monoamines — a different mechanism from single-target agents.
| Tesofensine (developmental code NS-2330) is a small-molecule triple monoamine reuptake inhibitor originally investigated for neurological indications before drawing intense interest for its pronounced metabolic effects. By blocking the reuptake transporters for dopamine, norepinephrine, and serotonin simultaneously, it raises the synaptic availability of all three — a broader central mechanism than agents that target a single transmitter.
At Guardian Labs, Tesofensine is supplied as a pre-mixed oral research solution standardized to 0.5 mg/mL, HPLC-verified and lot-verified, so concentration stays consistent across your appetite-regulation, metabolic, and neurochemical investigations. |
Most reuptake inhibitors act on one transporter. Tesofensine engages all three monoamine systems at once — the feature behind its distinctive research profile.
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Four defining features — a triple-transporter profile with a long tail.
i
Dopamine ReuptakeInhibits the dopamine transporter (DAT) with high potency — the pathway most associated with reward, motivation, and satiety signaling. |
ii
NorepinephrineBlocks the norepinephrine transporter (NET) most potently of the three, raising noradrenergic tone linked to energy expenditure. |
iii
SerotoninInhibits the serotonin transporter (SERT), the monoamine arm classically associated with satiety and mood regulation. |
iv
Long Half-LifeExhibits an unusually long plasma half-life of roughly 220 hours — a pharmacokinetic feature central to how it is studied and dosed. |
On the Triple Mechanism
Tesofensine’s reported transporter potencies run norepinephrine > dopamine > serotonin (IC₅₀ ≈ 1.7, 6.5, and 11 nM respectively). Engaging all three monoamine systems rather than one is what distinguishes it in appetite- and metabolism-focused research, and its ~220-hour half-life means steady-state behavior is a key variable in study design.
Primary subjects of investigation — strictly laboratory use.
A.01
Appetite RegulationStudies of monoamine-mediated satiety signaling, food intake, and body-weight regulation in metabolic models. |
A.02
Energy MetabolismResearch into noradrenergic effects on energy expenditure, thermogenesis, and metabolic rate. |
A.03
NeurochemistryInvestigating dopamine, norepinephrine, and serotonin transporter dynamics and synaptic availability. |
A.04
CNS & BehaviorExamining central monoamine signaling in motivation, reward, and behavioral models. |
Peer-reviewed literature supporting the research potential of this compound.
| i. |
Triple Monoamine Reuptake InhibitionPharmacology characterizing tesofensine as an inhibitor of the dopamine, norepinephrine, and serotonin transporters, establishing its triple-monoamine mechanism and relative transporter potencies. |
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| ii. |
Weight-Regulation Clinical Research (TIPO-1)A randomized controlled trial reporting dose-dependent reductions in body weight over 24 weeks in clinical study, framing tesofensine’s intensive interest as a metabolic research compound. |
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| iii. |
Appetite & Satiety MechanismsResearch examining tesofensine’s effects on appetite suppression and satiety signaling, attributing the effect to combined monoaminergic action in central feeding circuits. |
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| iv. |
Pharmacokinetics & Half-LifePharmacokinetic analysis characterizing tesofensine’s long plasma half-life (~220 hours) and the behavior of its active metabolite — a defining feature of its study design. |
