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

9 results

Linaclotide is a potent and selective guanylate cyclase C agonist that elicits pharmacological effects locally in the gastrointestinal tract.

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

Life sciences20 Mar 2010Cited by 148 (Europe PMC)

PMID20307554 (opens in a new tab)DOI10.1016/j.lfs.2010.03.015 (opens in a new tab)PepBankPUB-20307554
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 study9

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

  1. 01AnimalAnimal study (in vivo)Pharmacokinetics

    In the animal pharmacokinetic analysis, linaclotide oral bioavailability was 0.10%.

    In plain wordsIn animals, only 0.10% of oral linaclotide was bioavailable.

    Peptide
    Linaclotide
    Outcome
    Not applicableOral bioavailability
    Study

    n: not reported in source

    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 showed very low oral bioavailability (0.10%).
    1 context sentence
    Summary · context
    We determined the stability of linaclotide in the intestine, measured the oral bioavailability, and investigated whether the pharmacodynamic effects elicited in rodent models of gastrointestinal function are mechanistically linked to the activation of intestinal guanylate cyclase C (GC-C).
  2. 02AnimalAnimal study (in vivo)Efficacy outcome

    In wild-type mice, linaclotide significantly increased fluid secretion into ligated jejunal loops.

    In plain wordsIn mice with intact GC-C, linaclotide increased fluid secretion into intestinal loops.

    Peptide
    Linaclotide
    Outcome
    IncreaseIntestinal fluid secretion
    Study

    mousen: not reported in source

    Wild-type mice, ligated jejunal loops
    Outcome group
    Intestinal secretion · Gastrointestinal
    Studied dose
    Dose not stated

    Source sentences

    Summary
    In intestinal secretion and transit models, linaclotide exhibited significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops was accompanied by the secretion of elevated levels of cyclic guanosine-3',5'-monophosp…
  3. 03AnimalAnimal study (in vivo)Efficacy outcome

    In GC-C null mice, linaclotide did not significantly increase intestinal fluid secretion.

    In plain wordsIn mice without GC-C, linaclotide did not significantly increase intestinal fluid secretion.

    Peptide
    Linaclotide
    Outcome
    No significant changeIntestinal fluid secretion
    Study

    mousen: not reported in source

    GC-C null mice, ligated jejunal loops
    Outcome group
    Intestinal secretion · Gastrointestinal
    Studied dose
    Dose not stated

    Source sentences

    Summary
    In intestinal secretion and transit models, linaclotide exhibited significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops was accompanied by the secretion of elevated levels of cyclic guanosine-3',5'-monophosp…
  4. 04AnimalAnimal study (in vivo)Mechanism

    In wild-type mice, linaclotide increased cGMP secretion into ligated jejunal loops.

    In plain wordsIn mice with intact GC-C, linaclotide increased cGMP secretion into intestinal loops.

    Peptide
    Linaclotide
    Outcome
    IncreasecGMP secretion
    Study

    mousen: not reported in source

    Wild-type mice, ligated jejunal loops
    Outcome group
    Receptor activity and mechanism · Gastrointestinal
    Studied dose
    Dose not stated

    Source sentences

    Summary
    In intestinal secretion and transit models, linaclotide exhibited significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops was accompanied by the secretion of elevated levels of cyclic guanosine-3',5'-monophosp…
  5. 05AnimalAnimal study (in vivo)Mechanism

    In GC-C null mice, linaclotide lacked the significant cGMP secretion effect reported in wild-type mice.

    In plain wordsIn mice without GC-C, linaclotide lacked the cGMP secretion effect reported in normal mice.

    Peptide
    Linaclotide
    Outcome
    No significant changecGMP secretion
    Study

    mousen: not reported in source

    GC-C null mice
    Outcome group
    Receptor activity and mechanism · Gastrointestinal
    Studied dose
    Dose not stated

    Source sentences

    Summary
    In intestinal secretion and transit models, linaclotide exhibited significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops was accompanied by the secretion of elevated levels of cyclic guanosine-3',5'-monophosp…
  6. 06AnimalAnimal study (in vivo)Efficacy outcome

    In wild-type mice, linaclotide significantly accelerated gastrointestinal transit.

    In plain wordsIn mice with intact GC-C, linaclotide accelerated movement through the digestive tract.

    Peptide
    Linaclotide
    Outcome
    IncreaseGastrointestinal transit
    Study

    mousen: not reported in source

    Wild-type mice
    Outcome group
    Gastrointestinal motility · Gastrointestinal
    Studied dose
    Dose not stated

    Source sentences

    Summary
    In intestinal secretion and transit models, linaclotide exhibited significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops was accompanied by the secretion of elevated levels of cyclic guanosine-3',5'-monophosp…
  7. 07AnimalAnimal study (in vivo)Efficacy outcome

    In GC-C null mice, linaclotide did not significantly accelerate gastrointestinal transit.

    In plain wordsIn mice without GC-C, linaclotide did not significantly accelerate movement through the digestive tract.

    Peptide
    Linaclotide
    Outcome
    No significant changeGastrointestinal transit
    Study

    mousen: not reported in source

    GC-C null mice
    Outcome group
    Gastrointestinal motility · Gastrointestinal
    Studied dose
    Dose not stated

    Source sentences

    Summary
    In intestinal secretion and transit models, linaclotide exhibited significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops was accompanied by the secretion of elevated levels of cyclic guanosine-3',5'-monophosp…
  8. 08LabEx vivo tissueActivity measurement

    In wild-type mouse intestinal membranes, linaclotide inhibited radiolabeled STa binding in a concentration-dependent manner.

    In plain wordsIn lab tests, linaclotide reduced STa binding to normal mouse intestinal membranes as concentration increased.

    Peptide
    Linaclotide
    Outcome
    DecreaseSTa binding inhibition
    Study

    mousen: not reported in source

    Wild-type intestinal mucosal membranes
    Outcome group
    Receptor activity and mechanism · Gastrointestinal
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Linaclotide inhibited in vitro [(125)I]-STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner.

Studies that did not test the peptide alone1

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. 09LabNot a test of Linaclotide aloneIn vitro (cell-free)Pharmacokinetics

    In jejunal fluid in vitro, linaclotide completely degraded after 30 min.

    In plain wordsIn lab tests, linaclotide completely degraded after 30 min in jejunal fluid.

    Peptide
    Linaclotide
    Outcome
    Not applicableJejunal degradation
    Study

    n: not reported in source

    Jejunal fluid
    Outcome group
    Pharmacokinetics · Pharmacology

    Source sentences

    Summary
    After incubation in vitro in jejunal fluid for 30 min, linaclotide was completely degraded.

    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.

Registered trials1

Trials this study reports on, or that list this study as a reference. Registry data from ClinicalTrials.gov.

1 trial · 1 ongoing · source ClinicalTrials.gov (opens in a new tab)

RecruitingEarly phase 1NCT07569419

Proof of Principle Study for an Efficacy Trial of Linaclotide for Cystic Fibrosis

University of Nottinghamn = 269 Mar 2026 to est. Oct 2026

Cystic Fibrosis (CF)

Trial pageClinicalTrials.govUpdated 6 May 2026

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

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Terms as the source lists them.

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