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Related Concept Videos

Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
The Two-State Receptor Model01:29

The Two-State Receptor Model

The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with one...
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...
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...

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Related Experiment Video

Updated: Jul 27, 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

Opioid receptor regulation in mice

B C Yoburn1, B Billings, A Duttaroy

  • 1College of Pharmacy and Allied Health Professions, St. John's University, Queens, New York.

The Journal of Pharmacology and Experimental Therapeutics
|April 1, 1993
PubMed
Summary

Chronic opioid agonist and antagonist treatments in mice altered mu opioid receptor density, with naloxone increasing density and etorphine decreasing it. Opioid potency was not significantly affected by these treatments.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Opioid receptors are crucial for pain modulation.
  • Understanding how chronic opioid exposure affects receptor density is vital for managing pain and addiction.

Purpose of the Study:

  • To investigate the impact of chronic opioid agonist and antagonist administration on mu opioid receptor density and potency in a mouse model.

Main Methods:

  • Mice received chronic subcutaneous infusions or injections of etorphine, fentanyl, morphine, or naloxone for 7-8 days.
  • Mu opioid receptor density was assessed using [3H]DAMGO saturation binding assays.
  • Antinociceptive tolerance was evaluated via the tail-flick assay.

Main Results:

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Combining Laser Capture Microdissection and Microfluidic qPCR to Analyze Transcriptional Profiles of Single Cells: A Systems Biology Approach to Opioid Dependence
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Combining Laser Capture Microdissection and Microfluidic qPCR to Analyze Transcriptional Profiles of Single Cells: A Systems Biology Approach to Opioid Dependence

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Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
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  • Etorphine caused dose-dependent tolerance and mu opioid receptor downregulation.
  • Fentanyl infusions led to receptor upregulation at low doses and downregulation at high doses, with tolerance observed at the lowest dose.
  • Naloxone consistently increased mu opioid receptor density in a dose-dependent manner.
  • Morphine pellet implantation initially increased receptor density but had no effect after 7 days, despite observed tolerance.

    • Conclusions:

    • Chronic opioid administration differentially affects mu opioid receptor density, with agonists often causing downregulation and antagonists causing upregulation.
    • Observed changes in receptor density correlate with the development of antinociceptive tolerance.
    • Receptor affinity remained largely unaltered, suggesting density changes are the primary mechanism for altered potency.