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Record W2940964849 · doi:10.1002/prp2.475

The effect of chronic kidney disease on <scp>CYP</scp>2B expression and activity in male Wistar rats

2019· article· en· W2940964849 on OpenAlexafffund
Andrew S. Kucey, Thomas J. Velenosi, Nicholas C. Tonial, Alvin Tieu, Adrien A. E. RaoPeters, Bradley L. Urquhart

Bibliographic record

VenuePharmacology Research & Perspectives · 2019
Typearticle
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicPharmacogenetics and Drug Metabolism
Canadian institutionsLawson Health Research InstituteWestern University
FundersNatural Sciences and Engineering Research Council of CanadaCanada Foundation for Innovation
KeywordsKidney diseaseRenal functionPharmacokineticsEndocrinologyMetaboliteInternal medicineBupropionKidneyMedicinePharmacologyPopulationWestern blotChemistryPathologyBiochemistry

Abstract

fetched live from OpenAlex

Abstract Chronic kidney disease ( CKD ) is characterized by progressive reduction in kidney function over time. CKD affects greater than 10% of the population and its incidence is on the rise due to the growing prevalence of its risk factors. Previous studies demonstrated CKD alters nonrenal clearance of drugs in addition to reducing renal clearance. We assessed the function and expression of hepatic CYP 2B enzymes using a rat model of CKD . CKD was induced in Wistar rats by supplementing their chow with adenine and confirmed through the detection of elevated uremic toxins in plasma. Liver enzymes AST and ALT were unchanged by the adenine diet. Bupropion was used as a probe substrate for hepatic CYP 2B function using rat liver microsomes. The resulting metabolite, hydroxy‐bupropion, and bupropion were quantified by ultra‐performance liquid chromatography coupled to time‐of‐flight mass spectrometry. Level of mRNA and protein were determined by RT ‐ PCR and Western blot, respectively. The results of our study demonstrate that CYP 2B1 is downregulated in a rat model of CKD . CYP 2B1 mRNA level was significantly decreased (88%, P &lt; 0.001) in CKD relative to control. Similarly, maximal enzymatic velocity ( V max ) for CYP 2B was decreased by 46% in CKD relative to control ( P &lt; 0.0001). Previous studies involving patients with CKD demonstrated altered bupropion pharmacokinetics compared to control. Hence, our results suggest that these alterations may be mediated by attenuated CYP 2B hepatic metabolism. This finding may partially explain the alterations in pharmacokinetics and nonrenal drug clearance frequently observed in patients with CKD.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.005
metaresearch head score (Gemma)0.001
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow), Research integrity, Insufficient payload (model declined to judge)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.083
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0050.001
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0010.000
Bibliometrics0.0000.001
Science and technology studies0.0010.002
Scholarly communication0.0000.000
Open science0.0010.001
Research integrity0.0000.003
Insufficient payload (model declined to judge)0.0010.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.064
GPT teacher head0.468
Teacher spread0.404 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations8
Published2019
Admission routes2
Has abstractyes

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