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Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
Published on: July 29, 2014
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Recent Advances in Peripheral Opioid Receptor Therapeutics
Raghav Seth1, Sumanth S Kuppalli2, Danielle Nadav3
1Department of Anesthesia, Critical Care, and Pain Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, 330 Brookline Avenue, Boston, MA, 02215, USA. rseth@bidmc.harvard.edu.
Current Pain and Headache Reports
|May 10, 2021
Summary
New peripheral opioid receptor agonists offer pain relief while minimizing central side effects. Innovations include targeted delivery to inflamed tissues and reduced blood-brain barrier penetration, showing promise in animal models.
Area of Science:
- Pharmacology
- Pain Management
- Drug Development
Background:
- Opioids are effective analgesics but cause significant side effects, particularly for chronic pain.
- Centrally mediated side effects limit the utility of traditional opioid analgesics.
- Peripherally acting opioid receptor agonists aim to reduce these central adverse effects.
Purpose of the Study:
- To review recent advancements in peripheral opioid receptor therapeutics.
- To explore novel strategies for mitigating opioid side effects.
- To identify promising new peripheral opioid-based pain management strategies.
Main Methods:
- Review of recent scientific literature on peripheral opioid receptor agonists.
- Analysis of novel drug design approaches targeting peripheral opioid receptors.
- Evaluation of therapeutic strategies that limit blood-brain barrier penetration.
Main Results:
- Peripheral opioid receptor agonists effectively manage pain by targeting peripheral receptors.
- Novel therapeutics demonstrate reduced central nervous system activity.
- Examples include fentanyl-derived pH-sensitive ligands and bulky morphine conjugates.
- Promising results observed in preclinical animal models.
Conclusions:
- Recent innovations in peripheral opioid receptor therapeutics show significant potential.
- Targeted delivery and reduced blood-brain barrier permeability are key strategies.
- Further individualized testing is required to establish efficacy and safety in humans for specific chronic pain conditions.
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