Tesofensine (500mcg) Tablets x30

Overview

Tesofensine is a synthetic small-molecule compound belonging to the phenyltropane chemical class. It functions as a potent triple monoamine reuptake inhibitor (MRI), with high affinity for the transporters of dopamine (DAT), norepinephrine (NET), and serotonin (SERT). Originally investigated for neurodegenerative conditions such as Parkinson’s and Alzheimer’s disease, tesofensine was later repurposed in research targeting metabolic regulation and appetite suppression. Its multi-receptor activity makes it a valuable tool in laboratory studies examining energy balance, neurotransmitter signaling, and adaptive metabolic responses.

Chemical Structure

1. IUPAC Name: (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
2. Molecular Formula: C₁₇H₂₃Cl₂NO
3. Molecular Weight: ~328.3 Da
4. Core Scaffold: Phenyltropane backbone containing a dichlorophenyl group attached to an azabicyclic structure, with ethoxymethyl and methyl substituents.
5. Properties: Lipophilic design enabling efficient penetration of the blood–brain barrier and high-affinity interaction with monoamine transporters.

Research Background

Monoamine Modulation

1. Tesofensine inhibits presynaptic transporters for dopamine, norepinephrine, and serotonin, leading to sustained increases in extracellular monoamine concentrations.
2. This triple reuptake blockade supports studies on mood regulation, appetite control, and motivational pathways.

Metabolic & Appetite Studies

1. Laboratory and clinical investigations demonstrate tesofensine’s robust effect on reducing food intake through modulation of hypothalamic signaling circuits.
2. Research has shown dose-dependent reductions in body fat mass and total weight in metabolic studies.

Energy Expenditure

1. Preclinical findings report increased basal metabolic rate and enhanced fat oxidation, even under caloric restriction.
2. These effects position tesofensine as a compound of interest in studies of adaptive energy utilization.

Neurocognitive & Behavioral Exploration

1. Tesofensine has been studied in models assessing cognitive and behavioral function due to its broad monoaminergic activity.
2. Early data suggest possible links between monoamine modulation and neuroplasticity.

Safety & Observed Effects

1. Clinical and laboratory data have noted mild increases in heart rate and blood pressure, reflecting its noradrenergic activity.
2. These observations support continued investigation into dose-response relationships and safety considerations.

Areas of Scientific Interest

1. Triple monoamine transporter inhibition and neurotransmitter regulation.
2. Mechanisms of appetite suppression and feeding behavior.
3. Energy expenditure and fat oxidation pathways.
4. Neurocognitive and motivational effects of sustained monoamine modulation.
5. Cardiovascular and systemic markers associated with reuptake inhibition.

Citations

1. PubChem Compound Summary for Tesofensine (CID 11370864): molecular data—C₁₇H₂₃Cl₂NO; MW 328.3 Da. Overview of Tesofensine
2. JAMA Neurology: “Tesofensine (NS2330), a Monoamine Reuptake Inhibitor …” Preclinical and early human pharmacology. Overview of Tesofensine
3. The Lancet: Phase II clinical trial showing >20 lbs weight loss over 24 weeks and appetite-suppressant efficacy. Overview of Tesofensine
4. ScienceDirect Topics overview: “Tesofensine is a novel triple monoamine reuptake inhibitor … induces weight loss primarily by reducing food intake …” Overview of Tesofensine
5. PLOS ONE: “Tesofensine … silences GABAergic hypothalamic neurons,” demonstrating neuro-mechanistic appetite regulation. Overview of Tesofensine
6. The Peptide Report: “Tesofensine influences neurotransmitter levels to support metabolic health and cognitive function.” Overview of Tesofensine
7. HealthOn: Reports increased resting energy expenditure and metabolic rate during tesofensine use. Overview of Tesofensine
8. Biology Insights: “Tesofensine Side Effects: Neurological and Beyond” — details metabolic and cardiovascular side-effects. Overview of Tesofensine
9. PeptidesWiki: summarizing clinical trial outcomes in obesity, ADHD, and Parkinson's disease with neurobehavioral and safety data. Overview of Tesofensine