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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...
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...
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...
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. Thus, pain helps the...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that include the...

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Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels
16:36

Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels

Published on: May 18, 2009

P2X receptor ligands and pain.

Char-Chang Shieh1, Michael F Jarvis, Chih-Hung Lee

  • 1Dept. R4PM, Bldg. AP9A, Abbott Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA. char-chang.shieh@abbott.com

Expert Opinion on Therapeutic Patents
|February 11, 2010
PubMed
Summary

Purinergic P2X receptors, particularly P2X3, P2X4, and P2X7, are implicated in pain signaling. Targeting these receptors with small molecules shows promise for treating neuropathic and inflammatory pain.

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Chronic Post-Ischemia Pain Model for Complex Regional Pain Syndrome Type-I in Rats
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Chronic Post-Ischemia Pain Model for Complex Regional Pain Syndrome Type-I in Rats

Published on: January 21, 2020

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Last Updated: Jun 16, 2026

Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels
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Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels

Published on: May 18, 2009

Chronic Post-Ischemia Pain Model for Complex Regional Pain Syndrome Type-I in Rats
07:12

Chronic Post-Ischemia Pain Model for Complex Regional Pain Syndrome Type-I in Rats

Published on: January 21, 2020

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • P2X receptors are ligand-gated ion channels activated by extracellular nucleotides.
  • Seven P2X subunits (P2X1-7) exist, with P2X2, P2X3, P2X4, and P2X7 involved in nociception.
  • P2X3 receptors are in peripheral sensory neurons, while P2X4 and P2X7 are in immune cells.

Purpose of the Study:

  • To review recent literature and patents on P2X3, P2X4, and P2X7 receptors.
  • To explore small molecule ligands for potential pain therapeutics.
  • To understand the role of these receptors in nociceptive signaling and neuroinflammation.

Main Methods:

  • Gene silencing
  • Pharmacological studies
  • Electrophysiological approaches
  • Literature and patent review

Main Results:

  • P2X3 receptors mediate nociceptive signaling in peripheral neurons.
  • P2X4 and P2X7 receptors, expressed in immune cells, release pro-inflammatory cytokines.
  • Genetic disruption of P2X4 and P2X7 signaling reduces pain behaviors.

Conclusions:

  • P2X3, P2X4, and P2X7 receptors are key players in neuropathic and inflammatory pain.
  • Small molecule antagonists targeting these receptors represent a promising therapeutic strategy.
  • These receptors integrate neuroinflammation and pain pathways.