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Study · Animal study (in vivo) · rat · 2006

2 results

Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.

Samant MP, Hong DJ, Croston G, Rivier C, Rivier J

Journal of medicinal chemistry1 Jun 2006Cited by 11 (Europe PMC)

PMID16759096 (opens in a new tab)PMCIDPMC2536684 (opens in a new tab)DOI10.1021/jm060240a (opens in a new tab)PepBankPUB-16759096
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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 study2

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

  1. 01AnimalAnimal study (in vivo)Activity measurement

    In castrated male rats, no tested analogue matched the duration of action of degarelix.

    In plain wordsIn rats, no tested analogue matched the duration of action of degarelix.

    Peptide
    Degarelix
    Outcome
    IncreaseDuration of action
    Study

    ratn: not reported in source

    castrated male rat
    Comparator
    tested analogues
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    No analogue exhibited a duration of action comparable to that of degarelix.
    2 context sentences
    Summary · context
    Novel degarelix (Fe200486) analogues were screened for antagonism of GnRH-induced response (IC(50)) in a reporter gene assay.
    Summary · context
    Inhibition of luteinizing hormone release over time was measured in the castrated male rat.
  2. 02LabIn vitro (cells)Activity measurement

    In a reporter gene assay, degarelix had an IC(50) of 0.58 nM.

    In plain wordsIn lab tests, degarelix had an IC(50) of 0.58 nM for GnRH antagonism.

    Peptide
    Degarelix
    Outcome
    Not applicableGnRH antagonism IC50
    Study

    n: not reported in source

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

    Measurements

    IC50
    0.58 nM
    degarelix

    Source sentences

    Summary
    Analogues 8, 15-17, 22, and 23 were equipotent to acyline (IC(50) = 0.69 nM) and degarelix (IC(50) = 0.58 nM) in vitro.
    2 context sentences
    Summary · context
    Novel degarelix (Fe200486) analogues were screened for antagonism of GnRH-induced response (IC(50)) in a reporter gene assay.
    Summary · context
    Inhibition of luteinizing hormone release over time was measured in the castrated male rat.

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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

    28 Oct 2026, 02:03 UTC

    Study results updated

  2. Version 1

    27 Oct 2026, 16:34 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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