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Study · Non-randomized trial · 2014

4 results

Tesofensine, a novel triple monoamine re-uptake inhibitor with anti-obesity effects: dopamine transporter occupancy as measured by PET.

Appel L, Bergström M, Buus Lassen J, Långström B

European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology22 Oct 2013Cited by 27 (Europe PMC)

PMID24239329 (opens in a new tab)DOI10.1016/j.euroneuro.2013.10.007 (opens in a new tab)PepBankPUB-24239329
Publisher pagePubMedAsk about this study
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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study4

1 result from studies that gave the peptide. 1 result from people.

  1. 01HumanNon-randomized trialMechanism

    In a human PET study, tesofensine produced dose-dependent dopamine transporter blockade, with mean striatal occupancy ranging from 18% to 77%.

    In plain wordsIn a human PET study, tesofensine blocked more dopamine transporters at higher doses.

    Peptide
    Tesofensine
    Outcome
    IncreaseStriatal dopamine transporter occupancy
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Nervous system and cognition
    Studied dose
    0.125-1 mg · oral · 8-12 daysAs given in this study (human).

    Measurements

    Mean striatal DAT occupancy
    18 to 77%
    multiple tesofensine doses

    Source sentences

    Summary
    The mean striatal DAT occupancy varied dose-dependently between 18% and 77%.
    2 context sentences
    Summary · context
    The results demonstrated that TE induced a dose-dependent blockade of DAT following multiple doses of 0.125-1 mg TE at anticipated steady-state conditions.
    Summary · context
    This positron emission tomography (PET) study, using [¹¹C]βCIT-FE, aimed to assess the degree of the dopamine transporter (DAT) occupancy, at constant TE plasma levels, following different oral, multiple doses of TE during totally 8-12 days.

Studies that did not test the peptide alone3

In this study, Tesofensine was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Tesofensine.

  1. 02Computer modelNot a test of Tesofensine aloneIn silicoMechanism

    In a PET-data model, a sigmoid Emax relationship described striatal dopamine transporter occupancy versus tesofensine concentrations or doses.

    In plain wordsIn computer analysis, a model described dopamine transporter occupancy in relation to tesofensine concentrations or doses.

    Peptide
    Tesofensine
    Outcome
    Not applicableDAT occupancy model
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Nervous system and cognition

    Source sentences

    Summary
    A sigmoid E(max) model well described the relationship between striatal DAT occupancy and TE plasma concentrations or doses.
    1 context sentence
    Summary · context
    This positron emission tomography (PET) study, using [¹¹C]βCIT-FE, aimed to assess the degree of the dopamine transporter (DAT) occupancy, at constant TE plasma levels, following different oral, multiple doses of TE during totally 8-12 days.

    In this study, Tesofensine was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Tesofensine.

  2. 03Computer modelNot a test of Tesofensine aloneIn silicoMechanism

    In a PET-data model, estimated maximum dopamine transporter occupancy with tesofensine was about 80%.

    In plain wordsIn computer analysis, estimated maximum dopamine transporter occupancy with tesofensine was about 80%.

    Peptide
    Tesofensine
    Outcome
    Not applicableMaximum DAT occupancy
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Nervous system and cognition

    Measurements

    Maximum DAT occupancy
    ≈ 80%
    model estimate

    Source sentences

    Summary
    It was estimated that the maximum achievable DAT occupancy was about 80% and that half of this effect was accomplished by approximately 0.25 mg TE and a plasma drug concentration of 4 ng/ml.
    1 context sentence
    Summary · context
    This positron emission tomography (PET) study, using [¹¹C]βCIT-FE, aimed to assess the degree of the dopamine transporter (DAT) occupancy, at constant TE plasma levels, following different oral, multiple doses of TE during totally 8-12 days.

    In this study, Tesofensine was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Tesofensine.

  3. 04Computer modelNot a test of Tesofensine aloneIn silicoMechanism

    In a PET-data model, half-maximal tesofensine transporter occupancy corresponded to approximately 0.25 mg and a plasma concentration of 4 ng/ml.

    In plain wordsIn computer analysis, half-maximal transporter occupancy corresponded to approximately 0.25 mg tesofensine and 4 ng/ml in plasma.

    Peptide
    Tesofensine
    Outcome
    Not applicableHalf-maximal DAT occupancy
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Nervous system and cognition

    Measurements

    Half-maximal dose
    ≈ 0.25 mg
    tesofensine
    Half-maximal concentration
    4 ng/ml
    tesofensine

    Source sentences

    Summary
    It was estimated that the maximum achievable DAT occupancy was about 80% and that half of this effect was accomplished by approximately 0.25 mg TE and a plasma drug concentration of 4 ng/ml.
    1 context sentence
    Summary · context
    This positron emission tomography (PET) study, using [¹¹C]βCIT-FE, aimed to assess the degree of the dopamine transporter (DAT) occupancy, at constant TE plasma levels, following different oral, multiple doses of TE during totally 8-12 days.

    In this study, Tesofensine was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Tesofensine.

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

  1. Version 2Current

    21 Oct 2026, 15:58 UTC

    Study results updated

  2. Version 1

    21 Oct 2026, 12:50 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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