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Study · In vitro (cells) · 2019

4 results

Synthesis, Pharmacological, and Biological Evaluation of MIF-1 Picolinoyl Peptidomimetics as Positive Allosteric Modulators of D2R.

Sampaio-Dias IE, Silva-Reis SC, García-Mera X, Brea J, Loza MI, Alves CS, Algarra M, Rodríguez-Borges JE

ACS chemical neuroscience7 Aug 2019Cited by 10 (Europe PMC)

PMID31347842 (opens in a new tab)DOI10.1021/acschemneuro.9b00259 (opens in a new tab)PepBankPUB-31347842
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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

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

  1. 01LabIn vitro (cells)Activity measurement

    In cAMP mobilization assays with dopamine, MIF‑1 showed a bell-shaped dose-response curve and a response of 15.4 ± 5.5% at 0.1 nM.

    In plain wordsIn cells, MIF‑1 showed a bell-shaped response in the dopamine cAMP assay.

    Peptide
    MIF-1 (Pro-Leu-Gly-NH2)
    Outcome
    Not applicablecAMP mobilization modulation
    Study

    n: not reported in source

    D2 receptor functional assays
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    0.1 nMAs given in this study.

    Measurements

    cAMP assay response
    15.4%
    MIF-1 at 0.1 nM

    Source sentences

    Summary
    In this assay, 6b produced a typical bell-shaped dose-response curve similar to that of the parent neuropeptide (18.3 ± 7.1% for 6b vs 15.4 ± 5.5% for MIF-1, both at 0.1 nM).
    1 context sentence
    Summary · context
    Functional assays measuring cAMP mobilization in the presence of dopamine corroborate the activity of peptidomimetic 6b as a positive allosteric modulator (PAM) of D2R.
  2. 02LabIn vitro (cells)Activity measurement

    In receptor functional assays, dopamine EC50 with MIF‑1 was 0.17 ± 0.07 μM, comparable to 6b, both at 0.01 nM.

    In plain wordsIn lab tests, dopamine potency with MIF‑1 was comparable to that with compound 6b.

    Peptide
    MIF-1 (Pro-Leu-Gly-NH2)
    Outcome
    Not applicableDopamine EC50
    Study

    n: not reported in source

    D2 receptor functional assays
    Comparator
    compound 6b at 0.01 nM
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    0.01 nMAs given in this study.

    Measurements

    Dopamine EC50
    0.17 μM
    MIF-1 at 0.01 nM

    Source sentences

    Summary
    Dose-response curves for dopamine in the presence of 6b show EC50 (0.33 ± 0.21 μM for 6b vs 0.17 ± 0.07 μM for MIF-1) and Emax (86.0 ± 5.4% for 6b vs 93.6 ± 4.4% for MIF-1) comparable to those of MIF-1, both at 0.01 nM.
  3. 03LabIn vitro (cells)Activity measurement

    In receptor functional assays, dopamine Emax with MIF‑1 was 93.6 ± 4.4%, comparable to 6b, both at 0.01 nM.

    In plain wordsIn lab tests, the maximum dopamine response with MIF‑1 was comparable to that with compound 6b.

    Peptide
    MIF-1 (Pro-Leu-Gly-NH2)
    Outcome
    Not applicableDopamine maximal efficacy
    Study

    n: not reported in source

    D2 receptor functional assays
    Comparator
    compound 6b at 0.01 nM
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    0.01 nMAs given in this study.

    Measurements

    Dopamine Emax
    93.6%
    MIF-1 at 0.01 nM

    Source sentences

    Summary
    Dose-response curves for dopamine in the presence of 6b show EC50 (0.33 ± 0.21 μM for 6b vs 0.17 ± 0.07 μM for MIF-1) and Emax (86.0 ± 5.4% for 6b vs 93.6 ± 4.4% for MIF-1) comparable to those of MIF-1, both at 0.01 nM.
  4. 04LabIn vitro (cell-free)Activity measurement

    In receptor assays, MIF‑1 increased maximal tritiated NPA response by 18.3 ± 9.1% at 0.01 nM, close to the 6b effect.

    In plain wordsIn lab tests, MIF‑1 increased the maximum NPA response, with an effect close to compound 6b.

    Peptide
    MIF-1 (Pro-Leu-Gly-NH2)
    Outcome
    IncreaseMaximal NPA response
    Study

    n: not reported in source

    D2 receptor functional assays
    Comparator
    compound 6b at 0.01 nM
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    0.01 nMAs given in this study.

    Measurements

    Maximal NPA response increase
    18.3%
    MIF-1 at 0.01 nM

    Source sentences

    Summary
    Methyl picolinoyl-l-valyl-l-alaninate (compound 6b) produced a statistically significant increase in the maximal [3H]-NPA response at 0.01 nM (11.9 ± 3.7%), which is close to the effect of MIF-1 in this assay at same concentration (18.3 ± 9.1%).

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

    22 Oct 2026, 02:26 UTC

    Study results updated

  2. Version 1

    21 Oct 2026, 18:59 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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