Tesofensine is a next-generation triple serotonin, norepinephrine, and dopamine reuptake inhibitor (SNDRI) used in the treatment of obesity. Tesofensine acts primarily as an appetite suppressant, but possibly also increases resting energy expenditure. SNDRIs belong to the class of psychoactive antidepressants. They affect neurotransmitters in the brain, specifically serotonin, norepinephrine, and dopamine. Tesofensine's effects on the brain promote a feeling of maximum satiety during meals and significantly reduce appetite. Tesofensine also indirectly potentiates cholinergic neurotransmission and may have beneficial effects on cognition, particularly on learning and memory. Continuous treatment with tesofensine has been shown to increase BDNF levels in the brain and may possibly have an antidepressant effect.
Tesofensine was originally developed and patented by NeuroSearch A/S (Denmark) for the treatment of Parkinson's and Alzheimer's diseases. However, weight loss was consistently reported in the original studies, especially in overweight or obese patients; therefore, it was decided to develop tesofensine for the treatment of obesity.
Notably, tesofensine exhibits the following effects:
• It acts centrally, suppressing appetite, regulating the availability of dopamine receptors, and stimulating α1-adrenergic receptors.
• Appetite decreases within 14 days; there is a greater feeling of satiety and less desire to eat.
• It significantly increases fat oxidation and reduces adipose tissue.
• It improves insulin sensitivity, leading to higher glucose metabolism.
• It alters the expression of dopaminergic receptors in the cerebral striatum, as well as their binding.
• Energy consumption increases considerably within 14 days.
• The drug has a long half-life of 8 to 9 days and is primarily metabolized in the liver by CYP3A4 to the disalkylated metabolite M1 (NS-2360), which is the only metabolite found in human blood plasma.
Chemical name (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
Formula C17H23Cl2NO
Anabolic activity index is not a steroid.
Androgenic activity index is not a steroid.
Tesofensine is a next-generation triple serotonin, norepinephrine, and dopamine reuptake inhibitor (SNDRI) used in the treatment of obesity. Tesofensine acts primarily as an appetite suppressant, but possibly also increases resting energy expenditure. SNDRIs belong to the class of psychoactive antidepressants. They affect neurotransmitters in the brain, specifically serotonin, norepinephrine, and dopamine. Tesofensine's effects on the brain promote a feeling of maximum satiety during meals and significantly reduce appetite. Tesofensine also indirectly potentiates cholinergic neurotransmission and may have beneficial effects on cognition, particularly on learning and memory. Continuous treatment with tesofensine has been shown to increase BDNF levels in the brain and may possibly have an antidepressant effect.
Tesofensine was originally developed and patented by NeuroSearch A/S (Denmark) for the treatment of Parkinson's and Alzheimer's diseases. However, weight loss was consistently reported in the original studies, especially in overweight or obese patients; therefore, it was decided to develop tesofensine for the treatment of obesity.
Notably, tesofensine exhibits the following effects:
• It acts centrally, suppressing appetite, regulating the availability of dopamine receptors, and stimulating α1-adrenergic receptors.
• Appetite decreases within 14 days; there is a greater feeling of satiety and less desire to eat.
• It significantly increases fat oxidation and reduces adipose tissue.
• It improves insulin sensitivity, leading to higher glucose metabolism.
• It alters the expression of dopaminergic receptors in the cerebral striatum, as well as their binding.
• Energy consumption increases considerably within 14 days.
• The drug has a long half-life of 8 to 9 days and is primarily metabolized in the liver by CYP3A4 to the disalkylated metabolite M1 (NS-2360), which is the only metabolite found in human blood plasma.
Chemical name (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
Formula C17H23Cl2NO
Anabolic activity index is not a steroid.
Androgenic activity index is not a steroid.