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Study · Animal study (in vivo) · rat · 2011

5 results

Pharmacological characterization of FE 202158, a novel, potent, selective, and short-acting peptidic vasopressin V1a receptor full agonist for the treatment of vasodilatory hypotension.

Laporte R, Kohan A, Heitzmann J, Wisniewska H, Toy J, La E, Tariga H, Alagarsamy S, Ly B, Dykert J, Qi S, Wisniewski K and 4 more

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Galyean R, Croston G, Schteingart CD, Rivière PJ

The Journal of pharmacology and experimental therapeutics16 Mar 2011Cited by 31 (Europe PMC)

PMID21411496 (opens in a new tab)DOI10.1124/jpet.111.178848 (opens in a new tab)PepBankPUB-21411496
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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 study5

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

  1. 01AnimalAnimal study (in vivo)Activity measurement

    In rats, FE 202158 reduced ear skin blood flow, with a higher ED50 than AVP.

    In plain wordsIn rats, FE 202158 reduced ear skin blood flow, with a higher effective dose than AVP.

    Peptide
    Selepressin
    Outcome
    DecreaseEar skin blood flow
    Study

    ratn: not reported in source

    Comparator
    AVP
    Outcome group
    Blood pressure · Cardiovascular
    Studied dose
    Dose not stated · intravenous infusionAs given in this study (rat).

    Source sentences

    Summary
    and reduced rat ear skin blood flow after intravenous infusion in vivo (ED(50) = 4.0 versus 3.4 pmol/kg/min for AVP).
  2. 02AnimalAnimal study (in vivo)Activity measurement

    In rats, FE 202158 had a vasopressor effect as short as AVP at submaximally effective doses.

    In plain wordsIn rats, FE 202158 had a blood-pressure effect as short as AVP at the tested doses.

    Peptide
    Selepressin
    Outcome
    Not applicableVasopressor effect duration
    Study

    ratn: not reported in source

    Comparator
    AVP
    Outcome group
    Blood pressure · Cardiovascular
    Studied dose
    Dose not stated · intravenous bolusAs given in this study (rat).

    Source sentences

    Summary
    The duration of its vasopressor effect by intravenous bolus in rats was as short as AVP at submaximally effective doses.
  3. 03AnimalAnimal study (in vivo)Activity measurement

    In rats, FE 202158 lacked V2 receptor-mediated antidiuretic activity at its blood-flow ED50, unlike AVP.

    In plain wordsIn rats, FE 202158 lacked the urine-reducing activity seen with AVP at the tested dose.

    Peptide
    Selepressin
    Outcome
    Not applicableAntidiuretic activity
    Study

    ratn: not reported in source

    Comparator
    AVP
    Outcome group
    Kidney function · Kidney and urinary
    Studied dose
    Dose not stated · intravenous infusionAs given in this study (rat).

    Source sentences

    Summary
    FE 202158 had no V(2)R-mediated antidiuretic activity in rats by intravenous infusion at its ED(50) for reduction of ear skin blood flow, in contrast with the pronounced antidiuretic effect of AVP.
  4. 04LabEx vivo tissueActivity measurement

    In isolated rat iliac arteries, FE 202158 induced vasoconstriction with lower potency than AVP.

    In plain wordsIn lab tests, FE 202158 constricted rat arteries with lower potency than AVP.

    Peptide
    Selepressin
    Outcome
    IncreaseVasoconstriction
    Study

    ratn: not reported in source

    isolated common iliac artery
    Comparator
    AVP
    Outcome group
    Blood pressure · Cardiovascular
    Studied dose
    Dose not stated

    Source sentences

    Summary
    FE 202158 was a potent vasoconstrictor in the isolated rat common iliac artery ex vivo (EC(50) = 3.6 nM versus 0.8 nM for AVP)
  5. 05LabIn vitro (cells)Activity measurement

    In reporter assays, FE 202158 activated human V1a receptors with selectivity over V1b, V2 and oxytocin receptors.

    In plain wordsIn cells, FE 202158 activated human V1a receptors selectively over the other tested receptors.

    Peptide
    Selepressin
    Outcome
    IncreaseHuman V1a receptor agonism and selectivity
    Study

    n: not reported in source

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

    Source sentences

    Summary
    In functional reporter gene assays, FE 202158 was a potent and selective human V(1a)R agonist [EC(50) = 2.4 nM; selectivity ratio of 1:142:1107:440 versus human vasopressin type 1b receptor, vasopressin type 2 receptor (V(2)R), and oxytocin receptor, respectively]

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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 3Current

    27 Oct 2026, 18:20 UTC

    Study results updated

  2. Version 2

    27 Oct 2026, 16:32 UTC

    Study data updated · source update from Europe PMC

  3. Version 1

    9 Oct 2026, 02:52 UTC

    First added · source update from Europe PMC

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