Product Introduction
Name:Tesofensine
Product Benefits:Helps reduce appetite and weight
CAS:195875-84-4
Capacity:500mcg*100/bottle
Product Form:Tablets
Shelf Life:24 Months(The product packaging date shall prevail)
Introduction of Tesofensine
Tesofensine, also known as NS-2330, is a drug with potential anti-obesity effects. The following is a detailed introduction to Tesofensine:
1. Basic information
Chemical name: (1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
CAS number: There are multiple versions, such as 195875-84-4, 402856-42-2 and 13739-02-1, which may be due to differences in different production batches or different laboratory conditions.
Molecular formula: C17H23Cl2NO
Molecular weight: 328.27700
Density: 1.161 g/cm3 (or 1.18, data from different sources vary slightly)
Boiling point: 396.6ºC at 760 mmHg (or 247°C, which may be related to the purity of the compound or the test conditions)
Flash point: 193.7ºC
Appearance: white powder
2. Pharmacological action
Tesofensine is a triple monoamine reuptake inhibitor that effectively inhibits the reuptake of neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE; IC50=1.7 nM) and serotonin (5-HT; IC50=11 nM) in the synaptic cleft. This mechanism of action makes Tesofensine a potential anti-obesity agent because it can regulate appetite and energy expenditure by affecting these neurotransmitters.
3. Clinical application
Weight loss effect: Studies have shown that Tesofensine shows significant weight loss effects in obese patients. For example, in a Phase II study, obese patients lost a significant amount of weight on average after 24 weeks of Tesofensine treatment, and the weight loss effect was better than that of the diet and placebo groups.
Side effects: Although Tesofensine has a significant weight loss effect, it may also cause some side effects, such as mild nausea, diarrhea, constipation, insomnia, irritability, and increased heart rate. These side effects may increase the risk of heart disease in patients, so caution is required when using it.
4. Drug development and production
As a new type of weight loss drug, Tesofensine's development and production process needs to strictly comply with relevant laws and regulations. At present, some companies have begun to produce and sell Tesofensine or its related products, but the specific product quality and effect may vary from company to company. Therefore, when choosing and using Tesofensine, it is necessary to pay attention to factors such as the source, purity, and production process of the product.
5. Market and sales
Since Tesofensine has potential anti-obesity effects, it has received some attention in the market. However, since its side effects and safety issues have not been fully clarified, its marketing and sales are subject to certain restrictions. Currently, Tesofensine is mainly used in scientific research and clinical trial stages, and has not yet been widely used in clinical treatment.
How Tesofensine Works
Tesofensine is a norepinephrine, dopamine and 5-hydroxytryptamine reuptake inhibitor, and its specific mechanism of action is as follows:
1. Principle of action
Tesofensine exerts its pharmacological effects by regulating the activity of monoamine neurotransmitters (including dopamine, 5-hydroxytryptamine and norepinephrine). These neurotransmitters play a key role in regulating appetite, energy expenditure and metabolism. Tesofensine effectively suppresses appetite and promotes energy expenditure by enhancing POMC neuron activity and interfering with the midbrain reflux pathway.
2. Clinical research and efficacy
Clinical trial results: In a Phase II study published in The Lancet, Tesofensine showed significant efficacy in the treatment of obese patients. Compared with the placebo group, patients treated with Tesofensine had more significant weight loss in a dose-dependent manner.
Other efficacy: In addition to weight loss, Tesofensine also improved patients' glucose and lipid metabolism, reduced waist circumference, and showed the sustainability of weight loss in extended studies.
3. Precautions and potential risks
Cardiovascular and psychiatric reactions: Since Tesofensine acts on the monoamine system, it is necessary to pay attention to its possible adverse cardiovascular and psychiatric reactions, such as increased heart rate, changes in blood pressure, and symptoms such as depression and anxiety.
Long-term follow-up: For patients treated with Tesofensine, long-term follow-up should be performed to monitor its efficacy and safety.
Drug interactions: Tesofensine may interact with other drugs, so you should consult a doctor before use and inform all the drugs you are currently taking.
Tesofensine dosage and applicable population
Tesofensine is a serotonin, norepinephrine, and dopamine reuptake inhibitor. It was originally developed for the treatment of Parkinson's disease and Alzheimer's disease, and was later found to be useful for the treatment of obese patients. Here is some specific information about the dosage and applicable population of Tesofensine:
1. Dosage
Clinical trial dosage
In a Phase II study published in The Lancet, a total of 203 obese patients participated. They were randomly assigned to receive Tesofensine 0.25mg, 0.5mg, 1.0mg or placebo once a day for a total of 24 weeks.
Another study showed that low-dose Tesofensine is safe and effective in treating obesity. Specifically, the use of a 0.5mg dose of Tesofensine can produce a significant weight loss effect with only mild and transient adverse reactions.
Recommended dose
According to the report of Dr. Arne V. Astrup, head of the Department of Nutrition at the Faculty of Life Sciences of the University of Copenhagen, patients who received 0.25 mg of Tesofensine lost an average of 4.54% of their body weight, the 0.50 mg group lost 9.18%, and the 1.0 mg group lost 10.6%.
Dr. Arne V. Astrup suggested that 0.5 mg should be the recommended dose of Tesofensine, because the 1.0 mg dose did not cause more weight loss, but aggravated the adverse reactions.
2. Applicable population
Tesofensine is mainly used to treat obese patients, but the specific applicable population may vary from study to study. In general, the following groups may be suitable for the use of Tesofensine:
Obese patients: patients whose BMI (body mass index) exceeds the normal range and whose weight cannot be effectively controlled through diet control and physical exercise.
Patients without severe complications: patients with severe liver and kidney dysfunction, as well as patients with a history of epilepsy, should use Tesofensine with caution or avoid it.
3. Precautions
Adverse reactions: Tesofensine may cause increased blood pressure and increased heart rate, and the adverse reactions are proportional to the dose. Therefore, the patient's vital signs should be closely monitored during use.
Special populations: Pregnant women, lactating women, children under 18 years old, and the elderly should be particularly cautious when using Tesofensine. Animal experiments have observed that Tesofensine has teratogenic effects, so it is recommended that pregnant or pregnant women and lactating women should not take it. The dosage selection for children and the elderly should be adjusted according to specific circumstances.
Drug interactions: Tesofensine cannot be used simultaneously with monoamine oxidase inhibitors (MAOIs) to avoid drug interactions.
Benefits of Tesofensine
Tesofensine is a triple monoamine reuptake inhibitor. The following is an introduction to its advantages and applications:
1. Advantages
Tesofensine can effectively inhibit the reuptake of neurotransmitters dopamine, norepinephrine and serotonin in the synaptic cleft. This multiple inhibitory mechanism may give it unique advantages in the treatment of various diseases or conditions.
2. Applications
Since Tesofensine can regulate multiple neurotransmitters, it may have potential applications in the treatment of various diseases, including but not limited to:
Obesity: Tesofensine affects appetite and energy consumption by regulating neurotransmitters, which may help treat obesity.
Diabetes: Tesofensine may assist in the treatment of diabetes by improving insulin sensitivity and/or regulating glucose metabolism.
Mental illness: Tesofensine's regulatory effect on neurotransmitters may also make it potentially valuable in the treatment of certain mental illnesses (such as depression, anxiety, etc.).
However, the specific efficacy and safety of Tesofensine still need further clinical research and verification. When using Tesofensine, you should strictly follow the doctor's instructions and pay attention to monitoring the side effects and adverse reactions of the drug.
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FAQ
Q: What is Tesofensine?
A: Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor that effectively inhibits the reuptake of neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE; IC50=1.7 nM) and serotonin (5-HT; IC50=11 nM) in the synaptic cleft, and has potential anti-obesity effects.
Q: What is the main use of Tesofensine?
A: Tesofensine is a central nervous system-acting weight loss drug that helps reduce appetite and body weight by affecting the reuptake of neurotransmitters.
Q: What are the physical properties of Tesofensine?
A: The physical properties of Tesofensine include: density of 1.161 g/cm3, boiling point of 396.6ºC at 760 mmHg, and flash point of 193.7ºC. In addition, it also has certain stability and storage conditions requirements, and usually needs to be sealed and stored dry at 2-8°C.
Q: How effective is Tesofensine in animal experiments?
A: In animal experiments, Tesofensine exhibited significant anti-obesity effects. For example, in DIO rats, a single dose of Tesofensine (0.1-3 mg/kg, s.c.) strongly and dose-dependently suppressed food intake in DIO rats over 12 months. Daily administration of a moderate dose of Tesofensine (2.0 mg/kg, s.c.) for more than 16 days resulted in a significant decrease in body weight after 4 days of administration compared with a vehicle-treated control group.
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