Tesofensine (NS2330) (500mcg)

Tesofensine: The Triple Monoamine Modulator

Chemical Name: (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane Format: Oral Tablets Class: SNDRI (Serotonin-Norepinephrine-Dopamine Reuptake Inhibitor) Purity: ≥99% (HPLC) Half-Life: ~9 Days (Systemic)

Product Overview

Tesofensine (NS2330) is a novel, centrally acting triple monoamine reuptake inhibitor. Originally investigated for neurodegenerative conditions like Parkinson’s and Alzheimer’s, it was repurposed for metabolic research due to its profound effects on weight management and appetite suppression.

Unlike earlier agents that targeted only one or two neurotransmitters, Tesofensine simultaneously elevates Serotonin, Norepinephrine, and Dopamine in the synaptic cleft. This triple-action mechanism addresses the three pillars of metabolic optimization: increasing satiety, reducing food-seeking behavior, and enhancing the resting metabolic rate.

Mechanism of Action: Central Satiety & Thermogenesis

Tesofensine operates by modulating the chemical signals of hunger and energy expenditure in the brain.

• Triple Reuptake Inhibition: Blocks the transporters for Serotonin (SERT), Norepinephrine (NET), and Dopamine (DAT).

  • Serotonin: Increases feelings of fullness and satiety via POMC neurons.

  • Norepinephrine: Stimulates adrenergic pathways to increase metabolic expenditure and fat oxidation.

  • Dopamine: Normalizes reward circuitry, reducing the psychological drive for "hedonic" or compulsive eating.

• Hypothalamic Silencing: Research indicates that Tesofensine inhibits GABAergic neurons in the lateral hypothalamus (LH). Silencing these specific neurons reduces the initiation of feeding behaviors.

• Neurotrophic Support: Chronic treatment has been shown to increase levels of Brain-Derived Neurotrophic Factor (BDNF). This may help "reset" the biological body weight set-point and prevent the weight rebound common after caloric restriction.

Key Research Applications

1. Clinical Obesity & Weight Loss In Phase II trials (TIPO-1), the 500 mcg dose achieved a 9.2% weight loss over 24 weeks—approximately double the efficacy of many traditional agents. Research focuses on its ability to target visceral and abdominal fat specifically.

2. Metabolic Rate & Fat Oxidation Investigated for its ability to increase resting energy expenditure. Respiration chamber studies show that Tesofensine can increase 24-hour fat oxidation by 18 grams and boost nocturnal energy expenditure by 4.6%.

3. Hypothalamic Obesity & Rare Disorders Studied for its potential in treating resistant forms of obesity, such as Prader-Willi Syndrome and hypothalamic obesity, where the brain’s hunger-regulating centers are fundamentally impaired.

Storage & Handling

• Physical State: Oral tablets for precise research dosing.

• Storage: Store in a cool, dry place.

• Long-Term Storage: Store at -20°C (Freezer) to maintain maximum chemical stability.

• Stability: Highly lipophilic and stable at room temperature; however, it should be protected from light and moisture to prevent dealkylation.

Disclaimer

FOR RESEARCH USE ONLY. This product is a chemical compound intended strictly for laboratory research and development. It is not approved by the FDA for clinical use, diagnostics, or therapeutic procedures in humans or animals. The physiological and toxicological properties of this chemical have not been fully investigated.