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Related Concept Videos

Nociception01:44

Nociception

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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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Analgesia and Pain Management01:25

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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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GPCRs Regulate Adenylyl Cylase Activity01:09

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Inflammatory Response01:28

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An inflammatory response is a localized, nonspecific immune reaction that occurs when a tissue is injured. It is characterized by redness, swelling, heat, and pain, which are commonly called the cardinal signs and symptoms of inflammation. Inflammation can sometimes result in a loss of function.
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GPCR Desensitization01:12

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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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Opioid Receptors: Overview01:22

Opioid Receptors: Overview

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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,...
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Related Experiment Video

Updated: Jul 16, 2025

Chronic Post-Ischemia Pain Model for Complex Regional Pain Syndrome Type-I in Rats
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GPER involvement in inflammatory pain.

Baptiste Jouffre1, Alexandre Acramel2, Yves Jacquot3

  • 1Université Clermont Auvergne, Inserm U1107 Neuro-Dol, Pharmacologie Fondamentale et Clinique de la Douleur, Clermont-Ferrand, France; ANALGESIA Institute, Faculty of Medicine, 63000 Clermont-Ferrand, France.

Steroids
|September 21, 2023
PubMed
Summary

Chronic pain and inflammation are significant health issues. Targeting the G protein-coupled estrogen receptor (GPER) shows promise for new anti-inflammatory and pain relief therapies, offering an alternative to current treatments.

Keywords:
EstrogenGPERInflammationInflammatory painNociception

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Immunology

Background:

  • Chronic pain and inflammation represent a global health challenge with limited effective treatments.
  • Existing analgesics like opioids and NSAIDs have significant side effects.
  • The G protein-coupled estrogen receptor (GPER) is emerging as a key regulator of inflammatory pathways.

Purpose of the Study:

  • To investigate the role of G protein-coupled estrogen receptor (GPER) in inflammatory pain.
  • To evaluate the effects of GPER modulation on pain and inflammation in animal models.

Main Methods:

  • Pharmacological modulation of GPER in animal models of inflammatory pain.
  • Genetic modulation of GPER in animal models of inflammatory pain.
  • Analysis of GPER's direct actions on pain transmission and inflammation.

Main Results:

  • Pharmacological and genetic GPER modulation demonstrated significant effects on inflammatory pain.
  • Evidence suggests GPER influences both pain signaling and inflammatory processes.

Conclusions:

  • G protein-coupled estrogen receptor (GPER) modulation is a potential therapeutic strategy for inflammatory pain.
  • Further research into GPER mechanisms could lead to novel pain management treatments.