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tesofensine

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CAS:195875-84-4
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CAS:195875-84-4
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Products Intro: Product Name:(1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8- azabicyclo[3.2.1]octane
CAS:195875-84-4
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CAS:195875-84-4
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Products Intro: Product Name:Tesofensine
CAS:195875-84-4
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tesofensine Basic information
Product 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)-
CAS:195875-84-4
MF:C17H23Cl2NO
MW:328.28
EINECS:
Product Categories:
Mol File:195875-84-4.mol
tesofensine Structure
tesofensine Chemical Properties
Boiling point 396.6±42.0 °C(Predicted)
density 1.161±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMF: 2 mg/mL,DMSO: 1 mg/mL,Ethanol: Slightly soluble,PBS (pH 7.2): 0.14 mg/mL
form A solid
pka10.46±0.60(Predicted)
color White to off-white
Stability:Hygroscopic
InChIInChI=1S/C17H23Cl2NO/c1-3-21-10-14-13(9-12-5-7-17(14)20(12)2)11-4-6-15(18)16(19)8-11/h4,6,8,12-14,17H,3,5,7,9-10H2,1-2H3/t12-,13+,14+,17+/m0/s1
InChIKeyVCVWXKKWDOJNIT-ZOMKSWQUSA-N
SMILES[C@@]12([H])N(C)[C@@]([H])(CC1)C[C@H](C1=CC=C(Cl)C(Cl)=C1)[C@H]2COCC
Safety Information
MSDS Information
tesofensine Usage And Synthesis
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].
History 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].
UsesTesofensine, is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is currently in clinical development for the treatment of obesity.
References [1] Dourish, C. J. Wilding and J. Halford. “Anti-obesity Drugs: From Animal Models to Clinical Efficacy.”Animal and Translational Models for CNS Drug Discovery 2008: 271-315.
[2] Vidya Narayanaswami, Linda P. Dwoskin. “Obesity: Current and potential pharmacotherapeutics and targets.” Pharmacology Therapeutics 170 (2017): Pages 116-147.
tesofensine Preparation Products And Raw materials
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