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Study · Not a test of the peptide alone · 2008

6 results

Contribution of the active metabolite M1 to the pharmacological activity of tesofensine in vivo: a pharmacokinetic-pharmacodynamic modelling approach.

Lehr T, Staab A, Tillmann C, Nielsen EØ, Trommeshauser D, Schaefer HG, Kloft C

British journal of pharmacology5 Nov 2007Cited by 31 (Europe PMC)

PMID17982477 (opens in a new tab)PMCIDPMC2199391 (opens in a new tab)DOI10.1038/sj.bjp.0707539 (opens in a new tab)PepBankPUB-17982477
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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 study6

No result from this study comes from a test of the peptide.

Studies that did not test the peptide alone6

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. 01Computer modelNot a test of Tesofensine aloneIn silicoPharmacokinetics

    In mouse data, one-compartment models best described tesofensine and M1 pharmacokinetics.

    In plain wordsComputer analysis of mouse data described tesofensine and M1 with one-compartment models.

    Peptide
    Tesofensine
    Outcome
    Not applicablePharmacokinetic model
    Study

    mousen: not reported in source

    Mouse PK/PD model
    Outcome group
    Pharmacokinetics · Pharmacology

    Source sentences

    Summary
    Pharmacokinetics of tesofensine and M1 were best described by one-compartment models for both compounds.
    2 context sentences
    Summary · context
    Parent compound, metabolite and vehicle were separately administered intravenously and orally over a wide dose range (0.3-20 mg kg(-1)) to 228 mice.
    Summary · context
    Concentrations of tesofensine and M1 were measured; inhibition of the dopamine transporter was determined by co-administration of [(3)H]WIN35,428 as the pharmacodynamic measure.

    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. 02Computer modelNot a test of Tesofensine aloneIn silicoPharmacokinetics

    In mouse data, tesofensine and M1 showed nonlinear elimination kinetics with increasing dose.

    In plain wordsComputer analysis of mouse data found nonlinear elimination with increasing dose.

    Peptide
    Tesofensine
    Outcome
    Not applicableDose-dependent elimination
    Study

    mousen: not reported in source

    Mouse PK/PD model
    Outcome group
    Pharmacokinetics · Pharmacology

    Source sentences

    Summary
    Nonlinear elimination and metabolism kinetics were observed with increasing dose.
    2 context sentences
    Summary · context
    Parent compound, metabolite and vehicle were separately administered intravenously and orally over a wide dose range (0.3-20 mg kg(-1)) to 228 mice.
    Summary · context
    Concentrations of tesofensine and M1 were measured; inhibition of the dopamine transporter was determined by co-administration of [(3)H]WIN35,428 as the pharmacodynamic measure.

    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. 03Computer modelNot a test of Tesofensine aloneIn silicoPharmacokinetics

    In mouse data, tesofensine and M1 showed nonlinear metabolism kinetics with increasing dose.

    In plain wordsComputer analysis of mouse data found nonlinear metabolism with increasing dose.

    Peptide
    Tesofensine
    Outcome
    Not applicableDose-dependent metabolism
    Study

    mousen: not reported in source

    Mouse PK/PD model
    Outcome group
    Pharmacokinetics · Pharmacology

    Source sentences

    Summary
    Nonlinear elimination and metabolism kinetics were observed with increasing dose.
    2 context sentences
    Summary · context
    Parent compound, metabolite and vehicle were separately administered intravenously and orally over a wide dose range (0.3-20 mg kg(-1)) to 228 mice.
    Summary · context
    Concentrations of tesofensine and M1 were measured; inhibition of the dopamine transporter was determined by co-administration of [(3)H]WIN35,428 as the pharmacodynamic measure.

    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.

  4. 04Computer modelNot a test of Tesofensine aloneIn silicoPharmacokinetics

    An extended E(max) model described the tesofensine and M1 PK/PD relationship in mouse data.

    In plain wordsComputer analysis of mouse data described the concentration-effect relationship with an extended E(max) model.

    Peptide
    Tesofensine
    Outcome
    Not applicablePK/PD model
    Study

    mousen: not reported in source

    Mouse PK/PD model
    Outcome group
    Pharmacokinetics · Pharmacology

    Source sentences

    Summary
    The PK/PD relationship was described by an extended E(max) model.
    2 context sentences
    Summary · context
    Parent compound, metabolite and vehicle were separately administered intravenously and orally over a wide dose range (0.3-20 mg kg(-1)) to 228 mice.
    Summary · context
    Concentrations of tesofensine and M1 were measured; inhibition of the dopamine transporter was determined by co-administration of [(3)H]WIN35,428 as the pharmacodynamic measure.

    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.

  5. 05Computer modelNot a test of Tesofensine aloneIn silicoPharmacokinetics

    Effect compartments resolved observed hysteresis in the mouse tesofensine and M1 model.

    In plain wordsComputer analysis of mouse data used effect compartments to resolve delayed concentration-effect relationships.

    Peptide
    Tesofensine
    Outcome
    Not applicableHysteresis model
    Study

    mousen: not reported in source

    Mouse PK/PD model
    Outcome group
    Pharmacokinetics · Pharmacology

    Source sentences

    Summary
    Effect compartments were used to resolve observed hysteresis.
    2 context sentences
    Summary · context
    Parent compound, metabolite and vehicle were separately administered intravenously and orally over a wide dose range (0.3-20 mg kg(-1)) to 228 mice.
    Summary · context
    Concentrations of tesofensine and M1 were measured; inhibition of the dopamine transporter was determined by co-administration of [(3)H]WIN35,428 as the pharmacodynamic measure.

    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.

  6. 06Computer modelNot a test of Tesofensine aloneIn silicoActivity measurement

    In mouse data, tesofensine dopamine-transporter EC(50) values were lower than M1 values, which were 4-5-fold higher.

    In plain wordsComputer analysis of mouse data found lower concentrations for dopamine-transporter inhibition with tesofensine than with its M1 metabolite.

    Peptide
    Tesofensine
    Outcome
    DecreaseDopamine transporter inhibitory potency
    Study

    mousen: not reported in source

    Mouse PK/PD model
    Comparator
    M1 metabolite
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Measurements

    M1 EC(50) relative to tesofensine
    4 to 5 fold
    Dopamine transporter inhibition

    Source sentences

    Summary
    EC(50) values of M1, as an inhibitor of the dopamine transporter, were 4-5-fold higher than those for tesofensine in mice.
    2 context sentences
    Summary · context
    Parent compound, metabolite and vehicle were separately administered intravenously and orally over a wide dose range (0.3-20 mg kg(-1)) to 228 mice.
    Summary · context
    Concentrations of tesofensine and M1 were measured; inhibition of the dopamine transporter was determined by co-administration of [(3)H]WIN35,428 as the pharmacodynamic measure.

    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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