Evidence map›Paper›PMID 20942812›Full record

ArticleBritish journal of pharmacology2011

Biodistribution, pharmacokinetics and metabolism of interleukin-1 receptor antagonist (IL-1RA) using [¹⁸F]-IL1RA and PET imaging in rats.

C Cawthorne, C Prenant, A Smigova, P Julyan, R Maroy, K Herholz, N Rothwell, H Boutin

Open access · bronzeAbstract read
In one paragraph

Article in British journal of pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.

0numbers the graph read from it
0cells of the map it votes in
28citing papers in PubMed
3.2field-weighted citation impact, top 9% 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

28 citing papers in PubMed, 63 citations in OpenAlex.

  1. Can Nuclear Imaging Detect Trained Immunity in Cardiovascular Disease?Arteriosclerosis, thrombosis, and vascular biology · 2026
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  4. Measurement of Protein Synthesis Rate in Rat by [Molecular imaging and biology · 2023
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  8. Review
  9. Evaluation ofTheranostics · 2020
    Article
  10. Article
  11. Article
  12. Development & automation of a novel [(18)F]F prosthetic group, 2-[(18)F]-fluoro-3-pyridinecarboxaldehyde, and its application to an amino(oxy)-functionalised Aβ peptide.Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine · 2016
    Article
  13. Article
  14. IL-1α Gene Deletion Protects Oligodendrocytes after Spinal Cord Injury through Upregulation of the Survival Factor Tox3.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2015
    Article
  15. 18F-GE-180: a novel TSPO radiotracer compared to 11C-R-PK11195 in a preclinical model of stroke.European journal of nuclear medicine and molecular imaging · 2015
    Article
  16. Dynamic interactions between plasma IL-1 family cytokines and central endogenous opioid neurotransmitter function in humans.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2015
    Article
  17. Review
  18. Article
  19. Review
  20. Review
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

8 authors at 3 institutions in 2 countries.

C CawthorneWolfson Molecular Imaging Centre, University of Manchester, Manchester, UK.
C Prenant
A Smigova
P Julyan
R Maroy
K Herholz
N Rothwell
H Boutin
University of Manchester · GBCommissariat à l'Énergie Atomique et aux Énergies Alternatives · FRThe Christie Hospital · GB

Funding

Cancer Research UKMedical Research Council G0801296Medical Research Council G9219675
6 · The paper itself

Abstract

background and purposePositron emission tomography (PET) has the potential to improve our understanding of the preclinical pharmacokinetics and metabolism of therapeutic agents, and is easily translated to clinical studies in humans. However, studies involving proteins radiolabelled with clinically relevant PET isotopes are currently limited. Here we illustrate the potential of PET imaging in a preclinical study of the biodistribution and metabolism of ¹⁸F-labelled IL-1 receptor antagonist ([¹⁸F]IL-1RA) using a novel [¹⁸F]-radiolabelling technique. EXPERIMENTAL APPROACH: IL-1RA was radiolabelled by reductive amination on lysine moieties with [¹⁸F]fluoroacetaldehyde. Sprague-Dawley rats were injected intravenously with [¹⁸F]IL-1RA and imaged with a PET camera for 2 h. For the study of IL-1RA metabolites by ex vivoγ-counting of samples, rats were killed 20 min, 1 h or 2 h after injection of [¹⁸F]IL-1RA. KEY

results[¹⁸F]IL-1RA distribution into the major organs of interest was as follows: kidneys >> liver > lungs >> brain. In lungs and liver, [¹⁸F]IL-1RA uptake peaked within 1 min post-injection then decreased rapidly to reach a plateau from 10 min post-injection. In the brain, the uptake exhibited slower pharmacokinetics with a smaller post-injection peak and a plateau from 6 min onward. IL-1RA was rapidly metabolized and these metabolites represented ∼40% of total activity in plasma and ∼80% in urine, 20 min after injection. CONCLUSIONS AND IMPLICATIONS Preclinical PET imaging is a feasible method of assessing the biodistribution of new biological compounds of therapeutic interest rapidly. The biodistribution of [¹⁸F]IL-1RA reported here is in agreement with an earlier study suggesting low uptake in the normal brain, with rapid metabolism and excretion via the kidneys.

Indexed as

AnimalsAntirheumatic AgentsFluorine RadioisotopesHumansInterleukin 1 Receptor Antagonist ProteinMalePositron-Emission TomographyRatsRats, Sprague-DawleyAntirheumatic AgentsFluorine RadioisotopesInterleukin 1 Receptor Antagonist Protein

Identifiers

PMID20942812
PMCPMC3041255
OpenAlexW1569828475

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.