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tesofensine

tesofensine structure

tesofensine 

structure
  • CAS No:

    195875-84-4

  • Formula:

    C17H23Cl2NO

  • Chemical Name:

    tesofensine

  • Synonyms:

    (1S,3S,4R,5R)-3-(3,4-dichlorophenyl)-4-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane;(1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane;Tesofensine-13C-d3;8-Azabicyclo[3.2.1]octane, 3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-, (1R,2R,3S,5S)-;Tesofensine 500mcg Tablets;Tesofensine 0.5mg Tablets

  • Categories:

    Pharmaceutical Intermediates  >  Bulk Drug Intermediates

Description

Tesofensine ((1R, 2R, 3S, 5S)-3-(3, 4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane)) is an inhibitor of neuronal reuptake of dopamine, noradrenaline, and serotonin. Tesofensine was developed for the treatment of Alzheimer's and Parkinson's disease but lacked efficacy. Meta-analysis revealed that tesofensine (0.125–1.0 mg, once daily; oral) produced dose-dependent weight loss, and 32% of obese patients had ≥ 5% weight loss following 14 wk of treatment. Weight loss was accompanied by hypophagia, suggesting an appetite suppressant action[2].


Tesofensine is a dopamine, serotonin, and noradrenaline (triple) reuptake inhibitor originally developed by NeuroSearch for the treatment of Alzheimer's disease and Parkinson's disease. Development of the compound for these neurological indications was unsuccessful but significant weight loss was reported during the clinical trials in Parkinson's disease. Hence, tesofensine is now being developed by NeuroSearch for the treatment of obesity and type 2 diabetes[1].

tesofensine Basic Attributes

328.28

328.28

BLH9UKX9V1

White to off-white

Characteristics

1.161±0.06 g/cm3(Predicted)

396.6±42.0 °C(Predicted)

10.46±0.60(Predicted)

Store at -20°C

Drug Information

Investigated for use/treatment in alzheimer's disease, parkinson's disease, and obesity.

Tesofensine is a Serotonin-norepinephrine-dopamine-reuptake-inhibitor (SNDRI). SNDRIs are a class of psychoactive antidepressants. They act upon neurotransmitters in the brain, namely, serotonin, norepinephrine and dopamine. These three biogenic monoamines are associated with depression and increasing the availability in the brain is one method used to treat the condition.

(1R-(2-endo,3-exo))-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo(3,2,1)octane-2-hydroxy-1,2,3-propanetricarboxylate

tesofensine Use and Manufacturing

Tesofensine, is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is currently in clinical development for the treatment of obesity.

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