ArticleBritish journal of anaesthesia2019
BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates.
Article in British journal of anaesthesia, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 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
36 citing papers in PubMed, 54 citations in OpenAlex.
- Sex-Specific Relationships Between Nociceptin/Orphanin FQ Peptide (NOP) Receptors and Alcohol Drinking: Longitudinal PET Studies in Cynomolgus Monkeys.Basic & clinical pharmacology & toxicology · 2026Article
- Preclinical Evaluation of Dual NOP/Mu Partial Agonists for Methamphetamine Use Disorder.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Structural basis for dual targeting of μ-opioid and nociceptin/orphanin FQ receptors by Cebranopadol.Acta pharmacologica Sinica · 2026Article
- Article
- Synthesis and evaluation of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydromorphinone derivatives: mixed partial agonists at mu opioid and nociception/orphanin FQ peptide receptors.RSC medicinal chemistry · 2026Article
- Opioid-Induced Constipation: Mechanistic Insights, Experimental Models, and Future Perspectives.Biomedicines · 2026Review
- The Therapeutic Potential of Dual NMR (NOP/MOP) Agonism in Pain Management.Pain and therapy · 2026Review
- Breaking Through Cancer Pain: From Single-Drug Management to Multimodal Analgesia.Pain research & management · 2026Review
- Mu-opioid and nociceptin receptors show divergent, cell-type-specific actions in the mesocorticolimbic reward system in opioid use disorder.Frontiers in cellular neuroscience · 2026Review
- Buprenorphine Pharmacodynamics: A Bridge to Understanding Buprenorphine Clinical Benefits.Drugs · 2025Review
- Opioid system and related ligands: from the past to future perspectives.Journal of anesthesia, analgesia and critical care · 2024Review
- Signaling Modulation Mediated by Ligand Water Interactions with the Sodium Site at μOR.ACS central science · 2024Article
- Peptide-derived ligands for the discovery of safer opioid analgesics.Drug discovery today · 2024Review
- Review
- Activation of the nociceptin/orphanin-FQ receptor promotes NREM sleep and EEG slow wave activity.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Functional consequences of short-term exposure to opioids versus cannabinoids in nonhuman primates.Neuropharmacology · 2023Article
- PPL-138 (BU10038): A bifunctional NOP/mu partial agonist that reduces cocaine self-administration in rats.Neuropharmacology · 2022Article
- Current and Future Therapeutic Options in Pain Management: Multi-mechanistic Opioids Involving Both MOR and NOP Receptor Activation.CNS drugs · 2022Review
- Attenuated G protein signaling and minimal receptor phosphorylation as a biochemical signature of low side-effect opioid analgesics.Scientific reports · 2022Article
- Functional roles of neuromedin B and gastrin-releasing peptide in regulating itch and pain in the spinal cord of non-human primates.Biochemical pharmacology · 2022Article
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 3 countries.
Funding
Abstract
backgroundThe marked increase in mis-use of prescription opioids has greatly affected our society. One potential solution is to develop improved analgesics which have agonist action at both mu opioid peptide (MOP) and nociceptin/orphanin FQ peptide (NOP) receptors. BU10038 is a recently identified bifunctional MOP/NOP partial agonist. The aim of this study was to determine the functional profile of systemic or spinal delivery of BU10038 in primates after acute and chronic administration.
methodsA series of behavioural and physiological assays have been established specifically to reflect the therapeutic (analgesia) and side-effects (abuse potential, respiratory depression, itch, physical dependence, and tolerance) of opioid analgesics in rhesus monkeys.
resultsAfter systemic administration, BU10038 (0.001-0.01 mg kg
conclusionsThese in vivo findings demonstrate the translational potential of bifunctional MOP/NOP receptor agonists such as BU10038 as a safe, non-addictive analgesic with fewer side-effects in primates. This study strongly supports that bifunctional MOP/NOP agonists may provide improved analgesics and an alternative solution for the ongoing prescription opioid crisis.
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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.