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Related Concept Videos

Analgesia and Pain Management01:25

Analgesia and Pain Management

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Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
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Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
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Nociception—the ability to feel pain—is essential for an organism’s survival and overall well-being. Noxious stimuli such as piercing pain from a sharp object, heat from an open flame, or contact with corrosive chemicals are first detected by sensory receptors, called nociceptors, located on nerve endings. Nociceptors express ion channels that convert noxious stimuli into electrical signals. When these signals reach the brain via sensory neurons, they are perceived as pain.
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Research progress on the potential novel analgesic BU08028.

Ya Wang1, Di Qin2, Zhihua Guo1

  • 1School of Chemical Engineering, Changchun University of Technology, Changchun, 130012, China.

European Journal of Pharmacology
|December 7, 2021
PubMed
Summary

The novel opioid analog BU08028 shows promise as a safer analgesic with fewer adverse effects. It targets multiple receptors, potentially managing pain and addiction with reduced risks.

Keywords:
AnalgesicAnalgesic effectBU08028OpioidPain management

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Medicinal Chemistry

Background:

  • Pain management is crucial in treating various conditions, including cancer.
  • Traditional opioid analgesics present risks like dependence and adverse effects.
  • Developing safer alternatives with reduced addictive potential is a key research focus.

Purpose of the Study:

  • To review the development and characteristics of the novel opioid analog BU08028.
  • To summarize BU08028's analgesic efficacy, safety, and tolerance.
  • To explore BU08028's bifunctional activity and potential applications in pain and addiction management.

Main Methods:

  • Literature review of studies on BU08028.
  • Analysis of BU08028's interaction with mu opioid peptide (MOP) and nociceptin-orphanin FQ peptide (NOP) receptors.
  • Evaluation of preclinical data on analgesic effects, safety, and addiction-related properties.

Main Results:

  • BU08028 demonstrates fewer adverse effects compared to existing analgesics.
  • Its bifunctional action enhances MOP receptor-mediated analgesia while potentially mitigating opioid reward effects.
  • Studies suggest BU08028 may inhibit alcohol effects, indicating potential for alcohol addiction treatment.

Conclusions:

  • BU08028 represents a promising novel analgesic with a favorable safety profile.
  • Its dual-target mechanism offers unique advantages over single-target opioids.
  • BU08028 is a potential candidate for managing both pain and substance addiction.