Evidence map›Paper›PMID 29089037›Full record

ArticleFluids and barriers of the CNS2017

Revisiting atenolol as a low passive permeability marker.

Xiaomei Chen, Tim Slättengren, Elizabeth C M de Lange, David E Smith, Margareta Hammarlund-Udenaes

Open access · goldAbstract read
In one paragraph

Article in Fluids and barriers of the CNS, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
0.7field-weighted citation impact, top 27% 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

14 citing papers in PubMed, 28 citations in OpenAlex.

  1. Article
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  7. Fighting Plasmodium chloroquine resistance with acetylenic chloroquine analogues.International journal for parasitology. Drugs and drug resistance · 2022
    Article
  8. Review
  9. Article
  10. Article
  11. Understanding the brain uptake and permeability of small molecules through the BBB: A technical overview.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2021
    Review
  12. Article
  13. Review
  14. 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

5 authors at 3 institutions in 3 countries.

Xiaomei ChenDepartment of Pharmaceutical Biosciences, Translational PKPD Research Group, Uppsala University, Box 591, SE-75124, Uppsala, Sweden.
Tim SlättengrenDepartment of Pharmaceutical Biosciences, Translational PKPD Research Group, Uppsala University, Box 591, SE-75124, Uppsala, Sweden.
Elizabeth C M de LangeDepartment of Pharmacology, Leiden Academic Centre for Drug Research, Leiden, The Netherlands.
David E SmithDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, MI, 48109, USA.
Margareta Hammarlund-UdenaesDepartment of Pharmaceutical Biosciences, Translational PKPD Research Group, Uppsala University, Box 591, SE-75124, Uppsala, Sweden. mhu@farmbio.uu.se.ORCID http://orcid.org/0000-0002-9181-1321
Uppsala University · SECentre for Human Drug Research · NLUniversity of Michigan · US

Funding

Novel Transport and Activation Strategy to Improve the Bioavailability of Targeted ProdrugsR01GM115481 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI AMIDON, GORDON L, SMITH, DAVID E · 2015 to 2018
$1.7M
NIGMS NIH HHS R01 GM115481
6 · The paper itself

Abstract

backgroundAtenolol, a hydrophilic beta blocker, has been used as a model drug for studying passive permeability of biological membranes such as the blood-brain barrier (BBB) and the intestinal epithelium. However, the extent of S-atenolol (the active enantiomer) distribution in brain has never been evaluated, at equilibrium, to confirm that no transporters are involved in its transport at the BBB.

methodsTo assess whether S-atenolol, in fact, depicts the characteristics of a low passive permeable drug at the BBB, a microdialysis study was performed in rats to monitor the unbound concentrations of S-atenolol in brain extracellular fluid (ECF) and plasma during and after intravenous infusion. A pharmacokinetic model was developed, based on the microdialysis data, to estimate the permeability clearance of S-atenolol into and out of brain. In addition, the nonspecific binding of S-atenolol in brain homogenate was evaluated using equilibrium dialysis.

resultsThe steady-state ratio of unbound S-atenolol concentrations in brain ECF to that in plasma (i.e., K

conclusionsIt is concluded, based on K

Indexed as

AnimalsAtenololBlood-Brain BarrierCapillary PermeabilityMaleRatsRats, Sprague-DawleyAtenololAtenololBlood–brain barrierLipophilicityMicrodialysisPassive permeabilityPharmacokineticsTransportersUnbound equilibrium partition coefficient (Kp,uu,brain)Unbound volume of distribution in brain (Vu,brain)

Identifiers

PMID29089037
PMCPMC5664587
OpenAlexW2767110082

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.