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Opioid Receptors: Overview01:22

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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.
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Some receptors remain unoccupied even when an agonist produces a maximal response. Such empty ones are called spare receptors. In presence of spare receptors the maximum effect of an agonist drug is achieved with fewer than 100% of the receptors being occupied. To determine the presence of spare receptors, scientists often compare the concentration of the drug needed to produce 50% of the maximum effect (EC50) with the concentration of the drug needed to occupy 50% of the receptors (Kd). If the...
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Opioid Receptors.

Christoph Stein1,2

  • 1Department of Anesthesiology and Critical Care Medicine, Freie Universität Berlin, Charité Campus Benjamin Franklin, 12200 Berlin, Germany;

Annual Review of Medicine
|September 3, 2015
PubMed
Summary
This summary is machine-generated.

Opioids effectively treat severe acute and cancer pain. However, their long-term use for chronic pain requires careful consideration due to potential side effects and addiction risks.

Keywords:
addictioninflammationpainperipheralplasticitytolerance

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Pain Management

Background:

  • Opioids are potent analgesics with a long history of use.
  • Their application in acute and cancer pain is well-established.
  • Long-term use in chronic pain faces increasing scrutiny.

Purpose of the Study:

  • To review the mechanisms of opioid analgesia and other actions.
  • To discuss opioid receptors, ligands, and compounds.
  • To illustrate challenges in chronic pain management and addiction.

Main Methods:

  • Review of existing literature on opioid pharmacology and clinical use.
  • Discussion of opioid receptor structure, function, and plasticity.
  • Analysis of central and peripheral sites of opioid action and side effects.

Main Results:

  • Opioid receptors exhibit complex structures and functions.
  • Both central and peripheral sites mediate analgesia and side effects.
  • A range of endogenous and exogenous ligands interact with opioid receptors.
  • Conventional and novel opioid compounds offer diverse therapeutic options.

Conclusions:

  • Opioid efficacy is clear for severe acute and cancer pain.
  • Long-term opioid therapy for chronic pain presents significant challenges.
  • Understanding opioid mechanisms is crucial for managing pain and addiction.