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Drug Abuse and Addiction: Pharmacological Phenomena01:15

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Drug dependence, abuse, and addiction are complex phenomena that can precipitate various abnormal states. Physical dependence refers to a state of pharmacological adaptation to a drug. This adaptation often results in tolerance—a reduced response to the drug after repeated administrations. When the drug use is abruptly stopped, withdrawal symptoms occur due to the body's need to readjust from the pharmacologically induced imbalance. However, tolerance and withdrawal symptoms do not...
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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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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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Opioid Analgesics: Morphine and Other Natural Cogeners01:20

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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...
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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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Pain01:20

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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...
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Related Experiment Video

Updated: May 5, 2026

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
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A molecular basis for opiate action.

D Massotte1, B L Kieffer

  • 1Département des récepteurs et protéines membranaires, (CNRS UPR 9050), Ecole Supérieure de Biotechnologie de Strasbourg, Illkirch-Graffenstaden, France.

Essays in Biochemistry
|September 17, 1999
PubMed
Summary

Opioid receptors, crucial for pain relief and addiction, are now being studied at a molecular level. This research aims to develop non-addictive analgesics by understanding opioid receptor function.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Opioid receptors are key targets for pain management and understanding opiate addiction.
  • The endogenous opioid system involves peptides and three receptor types (mu, delta, kappa) regulating CNS functions like pain and mood.
  • Morphine is a primary example of an exogenous opiate acting on these receptors.

Purpose of the Study:

  • To explore the molecular mechanisms underlying opioid receptor action.
  • To leverage recent advances in opioid receptor cloning for novel research.
  • To pave the way for designing non-addictive analgesics.

Main Methods:

  • Utilizing in vitro structure-function studies of recombinant opioid receptors.
  • Employing in vivo gene targeting techniques.

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  • Applying molecular approaches for drug design.
  • Main Results:

    • The cloning of opioid receptors has enabled detailed molecular investigations.
    • Structure-function studies provide insights into receptor mechanisms.
    • Gene targeting offers a method to study receptor roles in vivo.

    Conclusions:

    • Molecular approaches are revolutionizing opioid research.
    • Understanding opioid receptor function is critical for developing safer pain therapeutics.
    • The goal is to create non-addictive analgesics by targeting the opioid system.