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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...
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 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...
GPCR Desensitization01:12

GPCR Desensitization

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...
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...
Desensitization and Tachyphylaxis01:20

Desensitization and Tachyphylaxis

Tachyphylaxis is described as a rapid decrease in response to a drug after repeated or continuous administration of the same drug dose. It is a phenomenon where the body becomes less responsive to a particular substance or intervention over time, requiring higher doses or stronger interventions to achieve the same effect. It results from adaptive changes in the body's receptors, signaling pathways, or physiological processes that occur in response to prolonged exposure to a stimulus.
Several...

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Related Experiment Video

Updated: May 24, 2026

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

[Protein kinase C and morphine tolerance].

Yu-Ping Huo1, Yan-Guo Hong

  • 1Key Laboratory of Developmental Biology and Neuroscience in Fujian Province, College of Life Sciences, Fujian Normal University, Fuzhou 350108, China.

Sheng Li Ke Xue Jin Zhan [Progress in Physiology]
|February 28, 2012
PubMed
Summary

Protein kinase C (PKC) is involved in morphine tolerance by desensitizing opioid receptors. Understanding PKC signaling is crucial for managing opioid tolerance clinically.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Context:

  • Protein kinase C (PKC) is a key enzyme in the AGC kinase family.
  • Morphine-induced desensitization of mu-opioid receptors (MOR) is linked to opioid tolerance.
  • PKC signaling pathways are implicated in cellular responses to opioids.

Purpose:

  • To review the role of Protein Kinase C (PKC) in the development and maintenance of morphine tolerance.
  • To explore the molecular mechanisms by which PKC influences mu-opioid receptor (MOR) desensitization.
  • To highlight the clinical significance of understanding PKC involvement in opioid tolerance.

Summary:

  • Protein kinase C (PKC) plays a critical role in the desensitization of mu-opioid receptors (MOR) following morphine administration.

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  • This desensitization process, mediated by PKC signaling, is a significant factor in the development and persistence of morphine tolerance.
  • The review consolidates current knowledge on PKC's involvement in opioid tolerance, emphasizing its potential as a therapeutic target.
  • Impact:

    • Provides a comprehensive overview of PKC's function in opioid tolerance.
    • Identifies PKC as a potential target for pharmacological interventions aimed at mitigating opioid tolerance.
    • Underscores the clinical relevance of PKC research for improving pain management strategies and reducing opioid dependence.