Tesofensine
$92.00 – $899.00
Tesofensine (NS2330) is a serotonin-norepinephrine-dopamine reuptake inhibitor derived from benztropine and is being developed for the treatment of obesity.
Description
Product Information:
Name: Tesofensine
CAS No.: 402856-42-2
Molecular Formula: C17H23NCl2O
Molecular Weight: 328.3
What is Tesofensine?
Tesofensine (NS2330) is a serotonin-norepinephrine-dopamine reuptake inhibitor derived from benztropine and is being developed for the treatment of obesity.
As of 2019, Tesofensine has been discontinued for the treatment of Alzheimer’s disease and Parkinson’s disease but is in phase III clinical trials for obesity.
Pharmacology
Metabolism and half-life
Tesofensine has a long half-life, about 9 days (220 hours), and is mainly metabolized by cytochrome P4503A4 (CYP3A4) to its dealkylated metabolite M1″NS2360. NS2360 is the only detectable metabolite in human plasma. It has a longer half-life of Bisofensine, which is about 16 days (374 hours) in the human body, and it exposes 31-34% of the parent compound at a steady state. In vivo data indicate that NS2360 is responsible for approximately 6% of Tesofensine’s activity. Like animals, the kidneys seem to play only a minor role (approximately 15-20%) in the elimination of Tesofensine from the human body.
Transporter selectivity
It was initially reported that the IC50 of Tesofensine under DAT, NAT, and 5HTT was 8.0, 3.2, and 11.0nM. However, the following data was recently submitted: IC50 (nM) NE 1.7, SER 11, DA 65. The revised IC50 will fully explain the lack of efficacy in the treatment of Parkinson’s disease, that is, the lack of efficacy of DRI compared to SERT and NET. This also helps explain why human stimulant abusers cannot reliably self-administer Tesofensine because it is believed that DAT inhibition is necessary, not NET inhibition.
Tesofensine also indirectly enhances cholinergic neurotransmission and has been shown to have a beneficial effect on cognition, especially in learning and memory. It has been shown that continuous treatment with Tesofensine increases BDNF levels in the brain and may have antidepressant effects.
Side effects
Common side effects include dry mouth, headache, nausea, insomnia, diarrhea, and constipation. Blood pressure and heart rate increased by 1-3 mmHg and 8 bpm, respectively. This is a promising new drug that has twice the weight loss effect of currently approved anti-obesity drugs.
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