Related Experiment Video

Updated: Aug 20, 2026

Dorsal Root Ganglia Isolation and Primary Culture to Study Neurotransmitter Release
08:15

Dorsal Root Ganglia Isolation and Primary Culture to Study Neurotransmitter Release

Published on: October 6, 2018

Neuropeptide FF (NPFF) analogs functionally antagonize opioid activities in NPFF2 receptor-transfected SH-SY5Y

Catherine Mollereau1, Honoré Mazarguil, Jean-Marie Zajac

  • 1Institut de Pharmacologie et de Biologie Structurale, CNRS, UMR 5089, 205 route de Narbonne, 31077 Toulouse cedex 04, France.

Molecular Pharmacology
|December 21, 2004
PubMed

Insights

Neuropeptide FF (NPFF) exhibits antiopioid activity by inhibiting cAMP production and modulating calcium channels. This study demonstrates NPFF

Area of Science:

  • Neuroscience
  • Pharmacology
  • Cell Biology

Background:

  • Neuropeptide FF (NPFF) is known to modulate opioid systems.
  • The SH-SY5Y neuroblastoma cell line expresses mu- and delta-opioid receptors.
  • Understanding NPFF's antiopioid mechanisms is crucial for pain management.

Purpose of the Study:

  • To elucidate the cellular antiopioid activity mechanism of neuropeptide FF (NPFF).
  • To characterize the interaction between NPFF receptors and opioid receptors in a transfected cell line.

Main Methods:

  • Transfection of SH-SY5Y cells with human NPFF2 receptor to create the SH2-D9 clone.
  • Assessment of receptor binding, cAMP production, and N-type Ca2+ channel activity.
  • Utilized G protein subunit-specific peptides to investigate receptor coupling.

Main Results:

  • The SH2-D9 clone expressed high-affinity NPFF2 receptors.
  • NPFF analog 1DMe inhibited forskolin-stimulated cAMP production and modulated opioid agonist effects on Ca2+ channels.
  • Demonstrated a 40% reduction in deltorphin-I's maximal effect by 1DMe, confirming antiopioid activity.
  • Identified coupling of NPFF2 receptors with Galphao and Galphai1,2 subunits mediating Ca2+ release.

Conclusions:

  • Neuropeptide FF (NPFF) exerts antiopioid effects through specific G protein coupling pathways.
  • The SH2-D9 cell line is a valuable model for studying NPFF and opioid receptor interactions.
  • This research provides insights into the molecular basis of NPFF's role in pain modulation.

More Related Videos

Dopamine Release at Individual Presynaptic Terminals Visualized with FFNs09:37

Dopamine Release at Individual Presynaptic Terminals Visualized with FFNs

Published on: August 31, 2009

Related Concept Videos

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, D-Pen5]-enkephalin or DPDPE for...
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...
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...
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates these...
NF-κB-dependent Signaling Pathway02:26

NF-κB-dependent Signaling Pathway

The transcription factor NF-κB was discovered in 1986 in the lab of Nobel laureate Professor David Baltimore, for its interaction with the immunoglobulin light chain enhancer in B-cells. After more than three decades of study, it is now evident that NF-κB regulates the expression of over 100 genes. Most of these genes play an essential role in the innate and adaptive immune responses as well as the inflammatory responses of animals.
NF-κB-dependent Signaling Mechanism
The heterodimer of NF-κB...
Drugs Affecting Neurotransmitter Synthesis01:29

Drugs Affecting Neurotransmitter Synthesis

Drugs affecting neurotransmitter synthesis can impact the adrenergic neuron and the synthesis of neurotransmitters. For example, α-methyltyrosine and carbidopa target specific enzymes involved in catecholamine synthesis. α-methyltyrosine inhibits the enzyme tyrosine hydroxylase, which converts tyrosine into dopamine. By blocking this enzyme, α-methyltyrosine reduces dopamine production and other catecholamines. Carbidopa, on the other hand, inhibits the enzyme dopa decarboxylase, which converts...