Related Experiment Video

Updated: Nov 28, 2025

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
07:23

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities

Published on: July 29, 2014

33.8K

Multifunctional Opioid-Derived Hybrids in Neuropathic Pain: Preclinical Evidence, Ideas and Challenges

Joanna Starnowska-Sokół1,2, Barbara Przewłocka1

  • 1Department of Pain Pharmacology, Maj Institute of Pharmacology, Polish Academy of Sciences, 31-343 Krakow, Poland.

Molecules (Basel, Switzerland)
|December 1, 2020
PubMed

Insights

New hybrid drugs combining opioids with other compounds show promise for treating neuropathic pain (NP). These dual-action therapies may improve efficacy and safety compared to traditional opioid agonists.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Drug Discovery

Background:

  • Neuropathic pain (NP) affects over half of patients unresponsive to first- and second-line treatments.
  • Opioid therapy for NP is often limited by pathological changes and adverse effects from compensatory mechanisms.
  • Pronociceptive neuropeptide systems activation counteracts opioid analgesia, necessitating higher doses and increasing side effects.

Purpose of the Study:

  • To review novel opioid-comprising hybrid drugs for neuropathic pain treatment.
  • To explore the biological actions, limitations, and challenges of these dually acting therapeutic approaches.
  • To highlight strategies for ameliorating NP treatment by addressing shared neuropathological mechanisms.

Main Methods:

  • Literature review of recent advancements in hybrid drug design for neuropathic pain.
  • Analysis of biological mechanisms underlying the efficacy and safety of opioid-based hybrid therapies.
  • Examination of challenges in developing and implementing these novel treatments.

Main Results:

  • Hybrid drugs combining opioid ligands with pharmacophores blocking anti-opioid actions offer a promising therapeutic strategy.
  • These dually acting agents can target shared neuropathological mechanisms in NP and opioid exposure.
  • Improved efficacy and safety profiles are anticipated compared to selective opioid agonists.

Conclusions:

  • Opioid-comprising hybrid drugs represent a rational design approach to enhance neuropathic pain management.
  • Addressing pronociceptive systems and opioid compensatory mechanisms is key to developing effective NP treatments.
  • Further research and development are needed to overcome limitations and challenges in this therapeutic area.
Keywords:
bifunctional designed ligandshybrid compoundsnerve injuryneuropathic painopioids

More Related Videos

Partial Sciatic Nerve Ligation: A Mouse Model of Chronic Neuropathic Pain to Study the Antinociceptive Effect of Novel Therapies08:16

Partial Sciatic Nerve Ligation: A Mouse Model of Chronic Neuropathic Pain to Study the Antinociceptive Effect of Novel Therapies

Published on: October 6, 2022

7.1K
The Sciatic Nerve Cuffing Model of Neuropathic Pain in Mice07:09

The Sciatic Nerve Cuffing Model of Neuropathic Pain in Mice

Published on: July 16, 2014

48.9K

Related Concept Videos

Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

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...
687
Analgesia and Pain Management01:25

Analgesia and Pain Management

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...
1.2K
Opioid Analgesics: Morphine and Other Natural Cogeners01:20

Opioid Analgesics: Morphine and Other Natural Cogeners

Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
618
Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2,...
3.3K
Nociception01:44

Nociception

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.
32.4K
Pain01:20

Pain

Pain serves as a critical warning signal that alerts the body to potential or actual harm. When mechanical pressure on the skin is intense, such as from a sharp pinch, the sensation transitions from touch to pain. Similarly, extreme temperatures, like a hot pot handle, convert the sensation of heat into pain. Pain can also result from overstimulation of other senses, such as blinding light, loud noise, or the intense heat from habañero peppers. This ability to sense pain is essential for...
1.0K