Related Experiment Video

Updated: Mar 26, 2026

The Sciatic Nerve Cuffing Model of Neuropathic Pain in Mice
07:09

The Sciatic Nerve Cuffing Model of Neuropathic Pain in Mice

Published on: July 16, 2014

49.7K

NPYFa, A Chimeric Peptide of Met-Enkephalin, and NPFF Induces Tolerance-Free Analgesia

Annu Mudgal1,2, Krishan Kumar1,3, Catherine Mollereau4,5

  • 1Peptide Synthesis Laboratory, CSIR-Institute of Genomics and Integrative Biology (CSIR-IGIB), New Delhi, India.

Chemical Biology & Drug Design
|January 24, 2016
PubMed

Insights

A novel chimeric peptide, NPYFa, demonstrates potent, long-lasting pain relief by targeting both opioid and neuropeptide FF receptors. Importantly, NPYFa does not lead to tolerance development, offering a promising new avenue for pain management.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Pain Research

Background:

  • Methionine-enkephalin-Arg-Phe is an endogenous analgesic peptide.
  • Neuropeptide FF (NPFF) modulates opioid effects and tolerance.
  • Understanding NPFF's role in opiate tolerance is crucial for pain management.

Purpose of the Study:

  • To design and characterize a chimeric peptide, NPYFa, targeting both opioid and NPFF receptors.
  • To evaluate the analgesic properties and receptor interactions of NPYFa.
  • To investigate the potential of NPYFa in preventing opiate tolerance.

Main Methods:

  • Synthesis of the chimeric peptide NPYFa (YGGFMKKKPQRFamide).
  • Assessment of antinociceptive effects in vivo.
  • Receptor binding studies using Eu-GTP-γS assay on cell lines expressing opioid and NPFF receptors.
  • Chronic treatment studies to evaluate tolerance development.

Main Results:

  • NPYFa induced potent, dose-dependent, and prolonged antinociception.
  • Antinociception was mediated via kappa-opioid receptors (KOR).
  • NPYFa demonstrated binding to both opioid and NPFF receptors.
  • Chronic NPYFa treatment did not result in tolerance development.

Conclusions:

  • NPYFa is a potent, long-acting antinociceptor with a unique dual-receptor targeting profile.
  • NPYFa lacks tolerance development, presenting a significant advantage over traditional opioids.
  • NPYFa serves as a valuable tool for investigating opioid analgesia and tolerance mechanisms.
Keywords:
chimeric peptideneuropeptide FFopiate tolerancetolerance-free antinociception

More Related Videos

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities07:23

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

Published on: July 29, 2014

34.3K
Electrophysiological Methods to Assess Peripheral Pain Block in an Anesthetized Rat07:58

Electrophysiological Methods to Assess Peripheral Pain Block in an Anesthetized Rat

Published on: November 21, 2025

271

Related Concept Videos

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...
2.9K
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.
34.6K
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...
1.4K
Local Anesthetics: Differential Sensitivity of Nerve Fibers01:24

Local Anesthetics: Differential Sensitivity of Nerve Fibers

Local anesthetics (LAs) block the sodium channels of nerve trunks, sensory nerve endings, and neuromuscular junctions. Although LAs can block all kinds of nerves, the sensitivity of nerve fibers differs according to nerve types and structures. LAs are known to block myelinated fibers faster than unmyelinated ones. Also, they block pain or sensory neurons at low concentrations without affecting the motor neurons involved in muscle contractions. This helps relieve labor pain without affecting the...
1.7K
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...
1.8K