NAV

Tesofensine

Targets (3)
This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Name
Tesofensine
Accession Number
DB06156
Description
Not Available
Type
Small Molecule
Groups
Investigational
Structure
Thumb
3D
Similar Structures
Weight
Average: 328.28
Monoisotopic: 327.1156698
Chemical Formula
C17H23Cl2NO
Synonyms
  • Tesofensine
External IDs
  • NS 2330
  • NS-2330

Pharmacology

Pharmacology
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Indication

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

Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics
Not Available
Mechanism of action

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.

TargetActionsOrganism
USodium-dependent serotonin transporterNot AvailableHumans
USodium-dependent noradrenaline transporterNot AvailableHumans
USodium-dependent dopamine transporterNot AvailableHumans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
Medicalerrors
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Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Tesofensine Citrate3R9T98ZB7U861205-83-6ZIVJUFNVDKADJT-BEDQTAKTSA-N
Tesofensine tartrate3H98FB5747Not AvailableRNHGKRXUMVFCTA-DRIRFIHHSA-N

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenyltropanes. These are compounds containing a phenyl group linked to a tropane moiety. Tropane is an organonitrogenous [3.2.1] bicyclic organic compound.
Kingdom
Organic compounds
Super Class
Alkaloids and derivatives
Class
Tropane alkaloids
Sub Class
Phenyltropanes
Direct Parent
Phenyltropanes
Alternative Parents
Phenylpiperidines / Dichlorobenzenes / Aralkylamines / N-alkylpyrrolidines / Aryl chlorides / Trialkylamines / Dialkyl ethers / Azacyclic compounds / Organopnictogen compounds / Organochlorides
show 1 more
Substituents
1,2-dichlorobenzene / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Chlorobenzene / Dialkyl ether
show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Chemical Identifiers

UNII
BLH9UKX9V1
CAS number
195875-84-4
InChI Key
VCVWXKKWDOJNIT-ZOMKSWQUSA-N
InChI
InChI=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
IUPAC Name
(1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
SMILES
CCOC[C@H]1[C@H]2CC[C@@H](C[C@@H]1C1=CC(Cl)=C(Cl)C=C1)N2C

References

General References
Not Available
ChemSpider
9545781
ChEMBL
CHEMBL3989690
ZINC
ZINC000003953158
Wikipedia
Tesofensine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentAlzheimer's Disease (AD)1
2CompletedTreatmentBMI >30 kg/m22
2CompletedTreatmentHypothalamic Injury-induced Obesity (HIO)1
2CompletedTreatmentParkinson's Disease (PD)3
2CompletedTreatmentPrader-Willi Syndrome1
2CompletedTreatmentType 2 Diabetes Mellitus1
1CompletedOtherHealthy Male Subjects1
1, 2CompletedTreatmentBMI >30 kg/m21

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000882 mg/mLALOGPS
logP4.95ALOGPS
logP4.16ChemAxon
logS-5.6ALOGPS
pKa (Strongest Basic)9.67ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity89.07 m3·mol-1ChemAxon
Polarizability35.36 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets
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Details1. Sodium-dependent serotonin transporter
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Serotonin:sodium symporter activity
Specific Function
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
Gene Name
SLC6A4
Uniprot ID
P31645
Uniprot Name
Sodium-dependent serotonin transporter
Molecular Weight
70324.165 Da
References
  1. Larsen MH, Rosenbrock H, Sams-Dodd F, Mikkelsen JD: Expression of brain derived neurotrophic factor, activity-regulated cytoskeleton protein mRNA, and enhancement of adult hippocampal neurogenesis in rats after sub-chronic and chronic treatment with the triple monoamine re-uptake inhibitor tesofensine. Eur J Pharmacol. 2007 Jan 26;555(2-3):115-21. Epub 2006 Oct 19. [PubMed:17112503]
Details2. Sodium-dependent noradrenaline transporter
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Norepinephrine:sodium symporter activity
Specific Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A2
Uniprot ID
P23975
Uniprot Name
Sodium-dependent noradrenaline transporter
Molecular Weight
69331.42 Da
References
  1. Larsen MH, Rosenbrock H, Sams-Dodd F, Mikkelsen JD: Expression of brain derived neurotrophic factor, activity-regulated cytoskeleton protein mRNA, and enhancement of adult hippocampal neurogenesis in rats after sub-chronic and chronic treatment with the triple monoamine re-uptake inhibitor tesofensine. Eur J Pharmacol. 2007 Jan 26;555(2-3):115-21. Epub 2006 Oct 19. [PubMed:17112503]
Details3. Sodium-dependent dopamine transporter
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Monoamine transmembrane transporter activity
Specific Function
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A3
Uniprot ID
Q01959
Uniprot Name
Sodium-dependent dopamine transporter
Molecular Weight
68494.255 Da
References
  1. Larsen MH, Rosenbrock H, Sams-Dodd F, Mikkelsen JD: Expression of brain derived neurotrophic factor, activity-regulated cytoskeleton protein mRNA, and enhancement of adult hippocampal neurogenesis in rats after sub-chronic and chronic treatment with the triple monoamine re-uptake inhibitor tesofensine. Eur J Pharmacol. 2007 Jan 26;555(2-3):115-21. Epub 2006 Oct 19. [PubMed:17112503]

Drug created on March 19, 2008 16:14 / Updated on February 21, 2021 18:52