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Study · Animal study (in vivo) · rat · 2010

8 results

Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit.

Busby RW, Bryant AP, Bartolini WP, Cordero EA, Hannig G, Kessler MM, Mahajan-Miklos S, Pierce CM, Solinga RM, Sun LJ, Tobin JV, Kurtz CB, Currie MG

European journal of pharmacology20 Sept 2010Cited by 172 (Europe PMC)

PMID20863829 (opens in a new tab)DOI10.1016/j.ejphar.2010.09.019 (opens in a new tab)PepBankPUB-20863829
Publisher pagePubMedAsk about this study
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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 study8

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

  1. 01AnimalAnimal study (in vivo)Pharmacokinetics

    In the pharmacokinetic analysis, linaclotide oral bioavailability was very low at 0.1%.

    In plain wordsIn animals, only 0.1% of oral linaclotide was bioavailable.

    Peptide
    Linaclotide
    Outcome
    Not applicableOral bioavailability
    Study

    n: not reported in source

    Pharmacokinetic analysis
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated · oralAs given in this study.

    Measurements

    Oral bioavailability
    0.1%
    oral administration

    Source sentences

    Summary
    Pharmacokinetic analysis of linaclotide showed very low oral bioavailability (0.1%).
    1 context sentence
    Summary · context
    We have characterized the solution structure of linaclotide, the in vitro binding and agonist activity to guanylate cyclase C receptors, the stability of linaclotide under conditions mimicking the gastric environment, oral bioavailability, and the pharmacodynamic effects in rat models of gastrointes…
  2. 02AnimalAnimal study (in vivo)Efficacy outcome

    In rats, oral linaclotide significantly increased gastrointestinal transit rates with dose at ≥5 μg/kg.

    In plain wordsIn rats, oral linaclotide increased movement through the digestive tract as dose increased.

    Peptide
    Linaclotide
    Outcome
    IncreaseGastrointestinal transit rate
    Study

    ratn: not reported in source

    Gastrointestinal transit model
    Outcome group
    Gastrointestinal motility · Gastrointestinal
    Studied dose
    ≥5 μg/kg · oralAs given in this study (rat).

    Source sentences

    Summary
    Orally administered linaclotide elicited a significant, dose-dependent increase in gastrointestinal transit rates in rats at doses of ≥5 μg/kg.
  3. 03AnimalAnimal study (in vivo)Efficacy outcome

    In rat intestinal loops, linaclotide significantly increased fluid secretion.

    In plain wordsIn rats, linaclotide increased fluid secretion into intestinal loops.

    Peptide
    Linaclotide
    Outcome
    IncreaseIntestinal fluid secretion
    Study

    ratn: not reported in source

    Surgically ligated small intestinal loops
    Outcome group
    Intestinal secretion · Gastrointestinal
    Studied dose
    Dose not stated · intestinal loop exposureAs given in this study (rat).

    Source sentences

    Summary
    Exposure of surgically ligated small intestinal loops to linaclotide induced a significant increase in fluid secretion, accompanied by a significant increase in intraluminal cGMP levels.
    1 context sentence
    Summary · context
    We have characterized the solution structure of linaclotide, the in vitro binding and agonist activity to guanylate cyclase C receptors, the stability of linaclotide under conditions mimicking the gastric environment, oral bioavailability, and the pharmacodynamic effects in rat models of gastrointes…
  4. 04AnimalAnimal study (in vivo)Mechanism

    In rat intestinal loops, linaclotide significantly increased intraluminal cGMP.

    In plain wordsIn rats, linaclotide increased cGMP inside intestinal loops.

    Peptide
    Linaclotide
    Outcome
    IncreaseIntraluminal cGMP
    Study

    ratn: not reported in source

    Surgically ligated small intestinal loops
    Outcome group
    Receptor activity and mechanism · Gastrointestinal
    Studied dose
    Dose not stated · intestinal loop exposureAs given in this study (rat).

    Source sentences

    Summary
    Exposure of surgically ligated small intestinal loops to linaclotide induced a significant increase in fluid secretion, accompanied by a significant increase in intraluminal cGMP levels.
    1 context sentence
    Summary · context
    We have characterized the solution structure of linaclotide, the in vitro binding and agonist activity to guanylate cyclase C receptors, the stability of linaclotide under conditions mimicking the gastric environment, oral bioavailability, and the pharmacodynamic effects in rat models of gastrointes…
  5. 05LabIn vitro (cells)Activity measurement

    In T84 cells, linaclotide showed high-affinity, pH-independent GC-C binding with Ki of 1.23-1.64 nM.

    In plain wordsIn cells, linaclotide bound strongly to GC-C receptors across pH conditions.

    Peptide
    Linaclotide
    Outcome
    Not applicableGC-C binding affinity
    Study

    humann: not reported in source

    T84 colon carcinoma cells
    Outcome group
    Receptor activity and mechanism · Gastrointestinal
    Studied dose
    Dose not stated

    Measurements

    Ki
    1.23 to 1.64 nM
    T84 cells

    Source sentences

    Summary
    Linaclotide exhibited high affinity and pH-independent binding (K(i): 1.23-1.64 nM) to guanylate cyclase C receptors on human colon carcinoma T84 cells and concomitantly, linaclotide binding resulted in a significant, concentration-dependent accumulation of intracellular cyclic guanosine-3', 5'-mono…
  6. 06LabIn vitro (cells)Mechanism

    In T84 cells, linaclotide significantly increased intracellular cGMP with concentration, with EC₅₀ of 99 nM.

    In plain wordsIn cells, linaclotide increased intracellular cGMP as its concentration increased.

    Peptide
    Linaclotide
    Outcome
    IncreaseIntracellular cGMP accumulation
    Study

    humann: not reported in source

    T84 colon carcinoma cells
    Outcome group
    Receptor activity and mechanism · Gastrointestinal
    Studied dose
    Dose not stated

    Measurements

    EC50
    99 nM
    cGMP accumulation

    Source sentences

    Summary
    Linaclotide exhibited high affinity and pH-independent binding (K(i): 1.23-1.64 nM) to guanylate cyclase C receptors on human colon carcinoma T84 cells and concomitantly, linaclotide binding resulted in a significant, concentration-dependent accumulation of intracellular cyclic guanosine-3', 5'-mono…

Studies that did not test the peptide alone2

In this study, Linaclotide 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 Linaclotide.

  1. 07LabNot a test of Linaclotide aloneIn vitro (cell-free)Pharmacokinetics

    In simulated gastric fluid at pH 1, linaclotide remained stable after 3 h incubation.

    In plain wordsIn lab tests, linaclotide remained stable for 3 h in simulated acidic stomach fluid.

    Peptide
    Linaclotide
    Outcome
    Not applicableGastric stability
    Study

    n: not reported in source

    Simulated gastric fluid, pH 1
    Outcome group
    Pharmacokinetics · Pharmacology

    Source sentences

    Summary
    Linaclotide was stable after 3 h incubation in simulated gastric fluid (pH 1) and similarly, was completely resistant to hydrolysis by pepsin.

    In this study, Linaclotide 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 Linaclotide.

  2. 08LabNot a test of Linaclotide aloneIn vitro (cell-free)Pharmacokinetics

    In laboratory tests, linaclotide completely resisted pepsin hydrolysis.

    In plain wordsIn lab tests, pepsin did not break linaclotide down.

    Peptide
    Linaclotide
    Outcome
    Not applicablePepsin resistance
    Study

    n: not reported in source

    Pepsin hydrolysis assay
    Outcome group
    Pharmacokinetics · Pharmacology

    Source sentences

    Summary
    Linaclotide was stable after 3 h incubation in simulated gastric fluid (pH 1) and similarly, was completely resistant to hydrolysis by pepsin.

    In this study, Linaclotide 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 Linaclotide.

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

    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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