ArticleMolecular pharmacology2017
Buprenorphine, Norbuprenorphine, R-Methadone, and S-Methadone Upregulate BCRP/ABCG2 Expression by Activating Aryl Hydrocarbon Receptor in Human Placental Trophoblasts.
Article in Molecular pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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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.
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Who cites it
19 citing papers in PubMed, 33 citations in OpenAlex.
- Review
- Interactions between long-acting antiretrovirals and opioids: a call for clinical awareness.Clinical microbiology reviews · 2026Review
- Targeting breast cancer resistance protein (BCRP/ABCG2) in cancer.Translational cancer research · 2024Review
- Effects of oxycodone on placental lineages: Evidence from the transcriptome profile of mouse trophoblast giant cells.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- The impact of opioids on the transcriptional landscape of human villous trophoblasts.Placenta · 2023Article
- An update on placental drug transport and its relevance to fetal drug exposure.Medical review (2021) · 2022Review
- The placenta as a target of opioid drugs†.Biology of reproduction · 2022Review
- Multidrug efflux transporter ABCG2: expression and regulation.Cellular and molecular life sciences : CMLS · 2021Review
- A review of the existing literature on buprenorphine pharmacogenomics.The pharmacogenomics journal · 2021Review
- Low oxygen tension differentially regulates the expression of placental solute carriers and ABC transporters.FEBS letters · 2021Article
- Transcriptomics and Other Omics Approaches to Investigate Effects of Xenobiotics on the Placenta.Frontiers in cell and developmental biology · 2021Review
- Maternal oxycodone treatment causes pathophysiological changes in the mouse placenta.Placenta · 2020Article
- Transcription factor-mediated regulation of the BCRP/Expert opinion on drug metabolism & toxicology · 2020Review
- Article
- Developing novel in vitro methods for the risk assessment of developmental and placental toxicants in the environment.Toxicology and applied pharmacology · 2019Review
- Regulation of human placental drug transporters in HCV infection and their influence on direct acting antiviral medications.Placenta · 2018Article
- An update on expression and function of P-gp/ABCB1 and BCRP/ABCG2 in the placenta and fetus.Expert opinion on drug metabolism & toxicology · 2018Review
- Interindividual Regulation of the Breast Cancer Resistance Protein/Drug metabolism and disposition: the biological fate of chemicals · 2018Article
- The Genomics of Neonatal Abstinence Syndrome.Frontiers in pediatrics · 2017Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Opioid dependence during pregnancy is a rising concern. Maintaining addicted pregnant women on long-acting opioid receptor agonist is the most common strategy to manage drug abuse in pregnant women. Methadone (MET) and buprenorphine (BUP) are widely prescribed for opiate maintenance therapy. Norbuprenorphine (NBUP) is the primary active metabolite of BUP. These medications can cross the placenta to the fetus, leading to postpartum neonatal abstinence syndrome. Despite their use during pregnancy, little is known about the cellular changes in the placenta brought about by these drugs. In this study, we showed that BUP, NBUP, and MET at clinically relevant plasma concentrations significantly induced BCRP mRNA up to 10-fold in human model placental JEG3 and BeWo cells and in primary human villous trophoblasts, and this induction was abrogated by CH223191, an aryl hydrocarbon receptor (AhR)-specific antagonist. These drugs increased AhR recruitment onto the AhR-response elements and significantly induced breast cancer resistance protein (BCRP) gene transcription. AhR overexpression further increased BCRP mRNA and protein expression. Knockdown of AhR by shRNA decreased BCRP expression, and this decrease was reversed by rescuing AhR expression. Finally, induction of BCRP expression in JEG3 and BeWo cells was accompanied by an increase in its efflux activity. Collectively, we have demonstrated, for the first time, that BUP, NBUP, and MET are potent AhR agonists and can induce BCRP in human placental trophoblasts by activating AhR. Given the critical role of BCRP in limiting fetal exposure to drugs and xenobiotics, long-term use of these medications may affect fetal drug exposure by altering BCRP expression in human placenta.
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Registered trials
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.