ArticleeLife2017
Polyglycerol-opioid conjugate produces analgesia devoid of side effects.
Article in eLife, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 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
18 citing papers in PubMed, 39 citations in OpenAlex.
- Effects of pH on opioid receptor activation and implications for drug design.Biophysical journal · 2024Review
- Hyperalgesic Effect Evoked by il-16 and its Participation in Inflammatory Hypernociception in Mice.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2024Article
- Nanotherapeutics for Alleviating Anesthesia-Associated Complications.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Review
- Targeting sensory neuron GPCRs for peripheral neuropathic pain.Trends in pharmacological sciences · 2023Review
- Peripheralization Strategies Applied to Morphinans and Implications for Improved Treatment of Pain.Molecules (Basel, Switzerland) · 2023Review
- Amelioration of injury-induced tissue acidosis by a nonsteroidal analgesic attenuates antinociceptive effects of the pH-dependent opioid agonist NFEPP.Scientific reports · 2022Article
- Targeting Neuroimmune Interactions in Diabetic Neuropathy with Nanomedicine.Antioxidants & redox signaling · 2022Article
- Recent Advances in Peripheral Opioid Receptor Therapeutics.Current pain and headache reports · 2021Review
- pKScientific reports · 2019Article
- [Pain inhibition by opioids-new concepts].Schmerz (Berlin, Germany) · 2019Review
- Current strategies toward safer mu opioid receptor drugs for pain management.Expert opinion on therapeutic targets · 2019Review
- [Pain inhibition by opioids-new concepts].Der Anaesthesist · 2019Review
- Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14- O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives.Journal of medicinal chemistry · 2019Article
- Article
- Opioid receptor signaling, analgesic and side effects induced by a computationally designed pH-dependent agonist.Scientific reports · 2018Article
- [Research consortium Neuroimmunology and pain in the research network musculoskeletal diseases].Zeitschrift fur Rheumatologie · 2018Review
- Advances in Achieving Opioid Analgesia Without Side Effects.Frontiers in pharmacology · 2018Review
- Inhibitory GMolecular painReview
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
14 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Novel painkillers are urgently needed. The activation of opioid receptors in peripheral inflamed tissue can reduce pain without central adverse effects such as sedation, apnoea, or addiction. Here, we use an unprecedented strategy and report the synthesis and analgesic efficacy of the standard opioid morphine covalently attached to hyperbranched polyglycerol (PG-M) by a cleavable linker. With its high-molecular weight and hydrophilicity, this conjugate is designed to selectively release morphine in injured tissue and to prevent blood-brain barrier permeation. In contrast to conventional morphine, intravenous PG-M exclusively activated peripheral opioid receptors to produce analgesia in inflamed rat paws without major side effects such as sedation or constipation. Concentrations of morphine in the brain, blood, paw tissue, and in vitro confirmed the selective release of morphine in the inflamed milieu. Thus, PG-M may serve as prototype of a peripherally restricted opioid formulation designed to forego central and intestinal side effects.
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.