ArticleJournal of lipid research2012
Cholesterol level influences opioid signaling in cell models and analgesia in mice and humans.
Article in Journal of lipid research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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.
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.
Who cites it
22 citing papers in PubMed, 37 citations in OpenAlex.
- Lipid profile dysregulation in opium users based on Fasa PERSIAN cohort study results.Scientific reports · 2021Trial
- Structural and dynamic studies uncover a distinct allosteric modulatory site at the µ-opioid receptor.Nature communications · 2026Article
- Structural and dynamic studies uncover a distinct allosteric modulatory site at the μ-opioid receptor.bioRxiv : the preprint server for biology · 2025Article
- Effects of Membrane Cholesterol on the Structure and Function of Selected Class A GPCRs─Challenges and Future Perspectives.Biochemistry · 2025Review
- Opioid-Modulated Receptor Localization and Erk1/2 Phosphorylation in Cells Coexpressing μ-Opioid and Nociceptin Receptors.International journal of molecular sciences · 2023Article
- Placental cytochrome P450 methylomes in infants exposed to prenatal opioids: exploring the effects of neonatal opioid withdrawal syndrome on health horizons.Frontiers in genetics · 2023Article
- Ptchd1 mediates opioid tolerance via cholesterol-dependent effects on μ-opioid receptor trafficking.Nature neuroscience · 2022Article
- Lipid rafts as viral entry routes and immune platforms: A double-edged sword in SARS-CoV-2 infection?Biochimica et biophysica acta. Molecular and cell biology of lipids · 2022Review
- Interaction With the Lipid Membrane Influences Fentanyl Pharmacology.Advances in drug and alcohol research · 2022Article
- Membrane cholesterol dependence of cannabinoid modulation of glycine receptor.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020Article
- Transcriptomic Analysis Reveals Receptor Subclass-Specific Immune Regulation of CD8ImmunoHorizons · 2020Article
- Association between perioperative cholesterol level and analgesia after video-assisted thoracoscopic surgery.Korean journal of anesthesiology · 2019Observational
- Is preoperative hypocholesterolemia a risk factor for severe postoperative pain? Analysis of 1,944 patients after laparoscopic colorectal cancer surgery.Journal of pain research · 2018Article
- Regulation of Pannexin 1 Surface Expression by Extracellular ATP: Potential Implications for Nervous System Function in Health and Disease.Frontiers in cellular neuroscience · 2017Article
- Article
- DMSO Enhances TGF-β Activity by Recruiting the Type II TGF-β Receptor From Intracellular Vesicles to the Plasma Membrane.Journal of cellular biochemistry · 2016Article
- Is hyperlipidemia a potential protective factor against intraoperative awareness in cardiac surgery?Journal of cardiothoracic surgery · 2016Review
- Opioid doses required for pain management in lung cancer patients with different cholesterol levels: negative correlation between opioid doses and cholesterol levels.Lipids in health and disease · 2016Article
- Membrane-Mediated Oligomerization of G Protein Coupled Receptors and Its Implications for GPCR Function.Frontiers in physiology · 2016Review
- Opioid receptors: toward separation of analgesic from undesirable effects.Trends in biochemical sciences · 2013Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
Cholesterol regulates the signaling of µ-opioid receptor in cell models, but it has not been demonstrated in mice or humans. Whether cholesterol regulates the signaling by mechanisms other than supporting the entirety of lipid raft microdomains is still unknown. By modulating cholesterol-enriched lipid raft microdomains and/or total cellular cholesterol contents in human embryonic kidney cells stably expressing µ-opioid receptor, we concluded that cholesterol stabilized opioid signaling both by supporting the lipid raft's entirety and by facilitating G protein coupling. Similar phenomena were observed in the primary rat hippocampal neurons. In addition, reducing the brain cholesterol level with simvastatin impaired the analgesic effect of opioids in mice, whereas the opioid analgesic effect was enhanced in mice fed a high-cholesterol diet. Furthermore, when the records of patients were analyzed, an inverse correlation between cholesterol levels and fentanyl doses used for anesthesia was identified, which suggested the mechanisms above could also be applicable to humans. Our results identified the interaction between opioids and cholesterol, which should be considered in clinics as a probable route for drug-drug interaction. Our studies also suggested that a low cholesterol level could lead to clinical issues, such as the observed impairment in opioid functions.
Indexed as
Identifiers
What OpenQuestion holds
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.