Tesofensine: Scientific Profile
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Monoamine reuptake inhibitor (NDRI) for research in weight-reduction models. It modulates the activity of the dopamine, norepinephrine, and serotonin transporters.
Tesofensine is a pharmacological agent composed of a tropane-derivative chemical structure, classified in the scientific literature as a triple monoamine reuptake inhibitor. Its biological activity centers on the competitive blockade of the synaptic transporters of serotonin (SERT), norepinephrine (NET) and dopamine (DAT), which increases the availability of these neurotransmitters in the synaptic cleft. In preclinical research models, this multichannel action has demonstrated a superior capacity for appetite suppression and modulation of basal energy expenditure compared with selective inhibitors.
The academic interest in Tesofensine lies in its prolonged half-life and its stable pharmacokinetic profile, which makes it possible to observe sustained metabolic effects over the long term. Current research explores its application in weight-reduction processes mediated by the hypothalamic control of hunger and satiety, as well as its influence on lipid oxidation. In addition to its effects on body mass, its potential impact on insulin sensitivity and other metabolic markers is being studied in experimental subjects with induced metabolic syndromes.
This compound is distinguished from other anorexigenic agents by a lower relative affinity toward the receptors that induce primary euphoria, which theoretically reduces the risk of abuse in controlled laboratory settings. Nonetheless, research must be carried out under strict surveillance owing to its potent effect on the sympathetic nervous system, which represents a critical area of study for determining its hemodynamic safety in various experimental models.
Mechanism of action
It acts by inhibiting the presynaptic reuptake of the three main monoaminergic neurotransmitters: dopamine, norepinephrine, and serotonin. By binding to the DAT, NET, and SERT transporters, Tesofensine prevents the removal of these ligands from the intersynaptic space, promoting persistent postsynaptic signaling. In the hypothalamus, this increase in monoamines modulates satiety circuits and thermogenic expenditure, resulting in a negative energy balance in the research model.
Mechanism summary
A triple reuptake inhibitor that increases dopamine, norepinephrine and serotonin levels to modulate satiety and metabolic expenditure.
Clinical Studies (6)
- Tesofensine, a novel antiobesity drug, silences GABAergic hypothalamic neurons (Perez CI et al. · PloS one · 2024) PMID 38656972.
- Tesofensine, a monoamine reuptake inhibitor for the treatment of obesity (Bello NT et al. · Current opinion in investigational drugs (London, England: 2000) · 2009) PMID 19777399.
- Tesofensine and weight loss (Tsai AG · Lancet (London, England) · 2009) PMID 19249625.
- Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial (Astrup, A, et al. · Lancet · 2008) PMID 18950853. [Con expresion de preocupacion editorial vigente. Interpretar con cautela.]
- Tesofensine, a novel triple monoamine reuptake inhibitor, induces appetite suppression by indirect stimulation of alpha1 adrenoceptor and dopamine D1 receptor pathways in the diet-induced obese rat (Axel, AM, et al. · Neuropsychopharmacology · 2010) PMID 20200509.
- The effect of the triple monoamine reuptake inhibitor tesofensine on energy metabolism and appetite in overweight and moderately obese men (Sjödin, A, et al. · International Journal of Obesity · 2010) PMID 20479765.
Warnings
Tesofensine is a research-use-only (RUO) compound; the following warnings and handling considerations apply to its laboratory use:
- Requires constant monitoring of cardiovascular parameters
- Not suitable for studies with preexisting hypertension models
- Controlled substance for academic research purposes only
- Concurrent use with monoamine oxidase inhibitors (MAOIs)
- History of cardiovascular disorders in the specimen
- Pregnancy or lactation in animal reproduction models
- Anxiety disorders or hypersensitivity to adrenergics
Technical data
- CAS
- 195875-84-4
- Molecular formula
- C17H23Cl2NO
- Molecular weight
- 328.28 Da
- Compound type
- nootropic
- Storage
- 15-25°C in a dry place
- Shelf life (lyophilized)
- 36 months
- Shelf life (reconstituted)
- Not applicable (tablet presentation)
- Light-sensitive
- No
Available for research
Tesofensine is available as a research reagent (RUO):
Frequently asked questions about Tesofensine
What is Tesofensine?
Monoamine reuptake inhibitor (NDRI) for research in weight-reduction models. It modulates the activity of the dopamine, norepinephrine, and serotonin transporters.
What is the mechanism of action of Tesofensine?
A triple reuptake inhibitor that increases dopamine, norepinephrine and serotonin levels to modulate satiety and metabolic expenditure.
What is Tesofensine researched for?
In preclinical research, Tesofensine is studied mainly in: Research on significant weight reduction; Study of appetite suppression at the hypothalamic level; Modulation of resting energy expenditure. Material exclusively for scientific research.
What are the chemical properties of Tesofensine?
Molecular formula C17H23Cl2NO; molecular weight 328.28 Da; CAS number 195875-84-4.
How is Tesofensine stored?
Storage conditions: 15-25°C in a dry place; lyophilized stability: 36 months; once reconstituted: Not applicable (tablet presentation).
What routes of administration are studied for Tesofensine?
In research models the following are described: Oral. Use is exclusively for scientific research.