Evidence map›Paper›PMID 17192834›Full record

ArticlePharmaceutical research2007

PEPT1 enhances the uptake of gabapentin via trans-stimulation of b0,+ exchange.

Theresa V Nguyen, David E Smith, David Fleisher

Abstract read
PubMed Publisher
In one paragraph

Article in Pharmaceutical research, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.3field-weighted citation impact, top 39% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed, 18 citations in OpenAlex.

  1. Review
  2. Article
  3. Di- and tripeptide transport in vertebrates: the contribution of teleost fish models.Journal of comparative physiology. B, Biochemical, systemic, and environmental physiology · 2017
    Review
  4. Article
  5. Article
  6. Article
  7. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

3 authors at 1 institution in 1 country.

Theresa V NguyenDeparment of Pharmaceutical Sciences, College of Pharmacy, The University of Michigan, 428 Church Street, Ann Arbor, Michigan 48109-1065, USA. tvnguyen@umich.edu
David E Smith
David Fleisher
University of Michigan–Ann Arbor · US

Funding

INTERDEPARTMENTAL TRAINING IN PHARMACOLOGICAL SCIENCEST32GM007767 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ISOM, LORI L. · 1985 to 2019
$10.2M
Role of PEPT2 in Peptide/Mimetic Disposition-DynamicsR01GM035498 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI SMITH, DAVID E · 1988 to 2013
$3.7M
NIGMS NIH HHS R01 GM035498NIGMS NIH HHS T32 GM007767
6 · The paper itself

Abstract

purposeThe aims of this study were (1) to determine whether amino acid and dipeptide loading can improve the effective permeability of gabapentin and (2) to characterize the underlying mechanism that is responsible for this interaction. MATERIALS AND

methodsAn in situ single-pass rat intestinal perfusion model was used to assess the effective permeability of gabapentin in rat, in the absence and presence of cellular loading by amino acid and dipeptide mixtures.

resultsCompared to gabapentin alone, cellular loading with amino acid and dipeptide mixtures significantly improved the effective permeability of gabapentin by 46-79% in jejunum and by 67-72% in ileum (p < or = 0.01). However, coperfusion of glycylsarcosine (i.e., PEPT1 substrate), methionine sulfoximine (i.e., glutamine synthase inhibitor), or lysine and arginine (i.e., b(0,+) substrates) with the amino acid and dipeptide mixtures compromised the intestinal uptake of gabapentin.

conclusionsThese findings demonstrate, for the first time, a direct relationship between the PEPT1-mediated uptake of a dipeptide and the trans-stimulated uptake of gabapentin (an amino acid-like drug) through the transport system b(0,+).

Indexed as

AminesAmino AcidsAmino Acid Transport SystemsAnimalsArginineBiological Transport, ActiveCyclohexanecarboxylic AcidsDipeptidesGabapentingamma-Aminobutyric AcidGlucoseGlutamate-Ammonia LigaseHydrogen-Ion ConcentrationIntestinal MucosaIntestinesLysineAminesAmino AcidsAmino Acid Transport SystemsArginineCyclohexanecarboxylic AcidsDipeptidesGabapentingamma-Aminobutyric AcidGlucoseGlutamate-Ammonia LigaseglycylsarcosineLysinePeptide Transporter 1SodiumSymportersWater

Identifiers

PMID17192834
OpenAlexW2078440910

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.