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Study · In vitro (cells) · 2006

4 results

Kinetic evidence for tandemly arranged ligand binding sites in melanocortin 4 receptor complexes.

Kopanchuk S, Veiksina S, Mutulis F, Mutule I, Yahorava S, Mandrika I, Petrovska R, Rinken A, Wikberg JE

Neurochemistry international9 Jun 2006Cited by 23 (Europe PMC)

PMID16764968 (opens in a new tab)DOI10.1016/j.neuint.2006.04.006 (opens in a new tab)PepBankPUB-16764968
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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

3 results from studies that gave the peptide. No result from this study comes from people.

  1. 01LabIn vitro (cells)Activity measurement

    Kinetic analysis of [(125)I]NDP-MSH binding to MC(4)R indicated heterogeneity, with binding to two tandemly arranged, interconnected binding sites.

    In plain wordsIn lab tests, NDP-MSH appeared to bind the MC(4)R receptor at two linked sites.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    Not applicableBinding kinetics of radiolabeled NDP-MSH at MC(4)R
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Kinetic analysis indicated heterogeneity in the binding of both radioligands, the binding apparently proceeding to two tandemly arranged interconnected mutually dependent binding sites.
    1 context sentence
    Summary · context
    The melanocortin 4 receptor (MC(4)R) binding of the peptide analogue of melanocyte stimulating hormone, [(125)I]NDP-MSH, and the low molecular weight radionucleid 1-(D-1,2,3,4-tetrahydroisoquinoline-3-carboxy-D-4-(125)iodophenylalanyl)-4-cyclohexyl-4-[(1,2,4-triazol-1-yl)methyl]piperidine trifluoroa…
  2. 02LabIn vitro (cells)Activity measurement

    When both receptor units had bound [(125)I]NDP-MSH, the radioligand could be released from only one unit, and the other stayed practically irreversibly bound.

    In plain wordsIn lab tests, once NDP-MSH filled both receptor units, it could leave only one unit and stayed stuck on the other.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    Not applicableRelease of bound [(125)I]NDP-MSH from receptor dimers
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    When both receptor units have bound [(125)I]NDP-MSH, the radioligand can be released only from one unit. The [(125)I]NDP-MSH bound to the remaining unit stays practically irreversibly bound due to a very slow retransformation rate of the transformed complex.
  3. 03LabIn vitro (cells)Activity measurement

    Adding NDP-MSH to the preformed [(125)I]THIQ-MC(4)R complex drastically retarded the release of [(125)I]THIQ.

    In plain wordsIn lab tests, adding NDP-MSH made another bound ligand leave the MC(4)R receptor much more slowly.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    Not applicableEffect of NDP-MSH on release of [(125)I]THIQ
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    addition of NDP-MSH as well as a fragment of the human agouti protein, hAGRP(83-132) to the preformed [(125)I]THIQ-MC(4)R complex drastically retarded the release of [(125)I]THIQ from the complex

Studies that did not test the peptide alone1

In this study, Melanotan I (afamelanotide) 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 Melanotan I (afamelanotide).

  1. 04LabNot a test of Melanotan I (afamelanotide) aloneIn vitro (cells)Activity measurement

    Apparent potencies of the same ligand differed by up to three orders of magnitude when assayed in competition with [(125)I]NDP-MSH or [(125)I]THIQ.

    In plain wordsIn lab tests, the measured strength of a ligand changed by up to a thousandfold depending on which radioligand was used.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    Not applicableApparent ligand potency with two radioligands
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    The consecutive binding of ligands to the MC(4)R dimers has substantial impact on the apparent ligand potencies, when determined in competition with the two different radioligands applied herein; the apparent potencies of the same ligand differing up to three orders of magnitude when assayed in comp…

    In this study, Melanotan I (afamelanotide) 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 Melanotan I (afamelanotide).

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

    13 Oct 2026, 21:44 UTC

    Study results updated

  2. Version 1

    13 Oct 2026, 16:31 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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