Description

Tesofensine Tablets – Product Details

Tesofensine
CAS Number	1208070-53-4
Molar Mass	328.3 g.mol-1
Chemical Formula	C17H23Cl2NO
IUPAC Name	(1R,2R,3S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane

What is Tesofensine?

Tesofensine is a new centrally acting triple monoamine reuptake inhibitor (MRI) that possesses an intrinsic inhibitory effect on the function of the transporters for norepinephrine (NE), serotonin (5-HT), and dopamine (DA).[R]

Tesofensine, which is known by its chemical name NS 2330, inhibits the reuptake of dopamine, serotonin, and norepinephrine. Indirectly, it stimulates the cholinergic system.

It has an extremely long half-life in humans, which is somewhere about eight days.

NS 2330 enhanced components of cognition, such as attention and the ability to retain and recall information, in a short phase II pilot research including patients with Alzheimer’s disease. The study lasted for 28 days and included dosages of 10.75 mg and 12.25 mg. NS 2330 may be able to improve motor function, mood, and cognition in people with Parkinson’s disease (PD) due to the pharmacologic actions that it carries out. [R]

This molecular compound indirectly stimulates the cholinergic system, and it works better than other weight loss agents.

Tesofensine is a reuptake inhibitor for noradrenaline, dopamine, and serotonin. It is being looked at as a drug to help people lose weight or fight obesity. It was first made as an antidepressant, but (pre-clinical) studies showed that it also helped people lose weight. [R]

What is Dopamine?

Dopamine is a neurotransmitter that plays a crucial role in several bodily functions. Its levels in the brain influence various functions, including mood, sleep, learning, movement, alertness, blood flow, and urine output.

Dopamine is involved in regulating mood, which means that low levels of dopamine can lead to feelings of depression and anxiety.

What is Serotonin?

Serotonin, also called 5-hydroxytryptamine (5-HT), is a key chemical messenger that helps the brain and other parts of the body do a lot of different things. As a neurotransmitter in the central nervous system (CNS), it is needed for several brain functions and is linked to anxiety and behavior.

Serotonin is also a major regulator of both how much energy is taken in and how much is used up. Serotonin in the central nervous system (CNS) plays a big role in hunger and food intake. This is a complicated process that has been studied a lot because serotonin makes people less hungry, and receptor agonists have been approved to treat obesity. [R]

What is Norepinephrine?

Norepinephrine (noradrenaline), produced mostly from sympathetic nerve fibers, increases heart rate and skeletal muscle contraction.

Norepinephrine helps the body prepare for a fight-or-flight reaction. Like other catecholamines, tyrosine produces norepinephrine.

Norepinephrine affects tissues via binding to α- and β-adrenergic receptors, or adrenoceptors, which react to adrenal hormones. It narrows blood arteries, raising blood pressure.

Norepinephrine increases blood pressure via increasing cardiac muscle output. Norepinephrine raises blood glucose and free fatty acids. It also modulates immune cell activity (e.g., T cells). Inactivation by COMT or MAO, reuptake into nerve terminals, or diffusion from binding sites efficiently terminates norepinephrine action. Norepinephrine that diffuses from nerve endings can activate distant adrenergic receptors. [R]

How Does Tesofensine Work?

It is abundantly clear that monoaminergic neurotransmission plays an important part in the homeostatic control of appetite sensations, and it is also apparent that there is a close link between the two.

Investigations that involve pharmacological manipulation, for example, have revealed that enhanced central monoaminergic activity induces dramatic effects on feeding behavior and, as a consequence, regulates the energy balance that is taken in by the body.

In addition, substances that increase synaptic levels of NE, 5-HT, or DA by increasing release or limiting reuptake in the synaptic terminals have the potential to decrease eating and weight gain.[R]

Tesofensine Research

Numerous animal and human studies have been conducted on the potential application of Tesofensine. Below are some of the relevant findings:

 Tesofensine for Type 2 Diabetes

The majority of people who are diagnosed with diabetes have type 2 diabetes mellitus, which accounts for 90 percent of all occurrences of diabetes worldwide.

As Tesofensine showed weight loss benefits, it is also currently being developed by NeuroSearch for the treatment of type 2 diabetes. The goal of the research is to investigate the drug’s safety and effectiveness in patients with type 2 diabetes mellitus.

Tesofensine on Obesity Treatment

A placebo-controlled trial was conducted to investigate the effectiveness of Tesofensine in reducing the desire for food, the amount of food consumed, and ultimately, body weight. Clinical trials were carried out on obese patients, where a reduction in weight was observed as a side effect.

The study involved 161 participants who received either 0.5 or 1.0 mg of tesofensine for 24 weeks. The results showed that research subjects started losing, those who received 0.5 mg lost an average of 11.3 kg, while those who received 1.0 mg lost an average of 12.8 kg. In contrast, the placebo group only saw a weight loss of 2.2 kg.

This suggests that tesofensine may be twice as effective in promoting significant weight loss as previously developed medications. The mechanism behind tesofensine’s promoting weight loss properties may be attributed to its ability to increase nocturnal energy expenditure and accelerate fatty acid oxidation. [R]

Moreover, tesofensine was found to improve glycemic control, insulin resistance, adiponectin levels, lipid profiles, and waist circumference. [R]

Does Tesofensine impact high blood pressure?

Tesofensine was linked to a number of side effects, the most prevalent of which were dry mouth, nausea, constipation, diarrhea, and firm stools. The research was carried out at five different centers for treating obesity in Denmark during phase II of a randomized, double-blind, placebo-controlled experiment. Although some study shows an increase in blood pressure, tesofensine 0.25 mg, and 0.5 mg did not produce significant increases in systolic or diastolic blood pressure when compared to the placebo group following a 2-week run-in period. [R]

Yet, these findings of safety and efficacy need to be confirmed in phase III clinical trials.

Tesofensine with Metoprolol

In a a study of diet-induced obese rats were given tesofensine, which is used to treat obesity, and metoprolol, which is used to treat high blood pressure. The results showed that treatment with tesofensine alone led to a lot of weight loss and less food intake, but it also caused bad effects on the heart and blood vessels, like a faster heart rate and higher blood pressure. But when tesofensine was combined with metoprolol, its effects on weight loss and suppressing the appetite were kept while its bad effects on the heart were stopped.

Overall, it looks like the combination of tesofensine and metoprolol is a good way to treat obesity without hurting the health of the heart. Even though the study showed promising results when tesofensine and metoprolol were used together to treat rats, more tests need to be done to see if this combination is safe and effective for people. [R]

It is also important to think about possible side effects and drug interactions that could happen if these medicines are taken at the same time. Further studies are also recommended to understand the full effect of tesofensine and metoprolol.

 

Tesofensine on Parkinson’s or Alzheimer’s disease

Brain-derived neurotrophic factors (BDNFs) are important for keeping synapses flexible, which is important for learning and remembering in Alzheimer’s disease. Tesofensine has been proven in experiments both in vitro and in vivo to decrease or inhibit neurotransmitter presynaptic reuptake of the neurotransmitters serotonin, norepinephrine, and dopamine.

Acetylcholine, noradrenaline, and dopamine are all neurotransmitters that are affected by Alzheimer’s disease (neurological conditions), and the molecule improves the function of all three of these neurotransmitters. After administering tesofensine to mice, research shows that there was a reduction in the quantity of beta-amyloid, which was assumed to be a neuroprotective effect. [R]

  

Tesofensine on Addiction (Mental Health Research)

Tesofensine and other drugs that block the reuptake of monoamines have worked well in animal models of addiction. This is because dopamine is linked to the reward system and the behaviors that go along with it. Agents that specifically block dopamine reuptake, like tesofensine, may be more effective in treating substance use disorders. This is because dopamine is a key part of the brain’s reward circuitry and behaviors related to addiction. [R]

Still, more research is needed to find out the pros and cons of using these drugs to treat addiction in human models as it was found to have better effects in animal models.

Summary Tesofensine

Tesofensine is a triple monoamine reuptake inhibitor that inhibits the reuptake of dopamine, serotonin, and norepinephrine, and indirectly stimulates the cholinergic system. It has a long half-life in humans and may improve motor function, mood, and cognition in people with Parkinson’s disease. It is being researched as a potential weight loss drug as it helps induce appetite suppression and controls eating behavior.

Is Tesofensine for Research Purposes Only?

In addition to a lack of consistent evidence of direct benefits, the potential long-term effects of tesofensine are also unknown.

Purerawz sells tesofensine for research purposes(lab supply) only.

Where to buy Tesofensine Online

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Disclaimer

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