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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...
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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: Synthetic and Semisynthetic Opioids

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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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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.
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Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis
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Dynorphin peptides differentially regulate the human kappa opioid receptor.

Yong Chen1, Chongguang Chen, Lee-Yuan Liu-Chen

  • 1Department of Pharmacology and Center for Substance Abuse Research, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, U.S.A.

Life Sciences
|February 24, 2007
PubMed
Summary

Dynorphin A and B significantly down-regulate the kappa opioid receptor (KOR), while alpha-neoendorphin causes less adaptation. Peptide stability and intrinsic properties influence these differential KOR regulations.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Molecular Biology

Background:

  • Dynorphins are endogenous peptides acting on the kappa opioid receptor (KOR).
  • These peptides are involved in various physiological and pathological processes.
  • Understanding their regulation of KOR is crucial for therapeutic development.

Purpose of the Study:

  • To investigate the differential regulation of the human kappa opioid receptor (hKOR) by three major prodynorphin peptides: dynorphin A (1-17) (Dyn A), dynorphin B (1-13) (Dyn B), and alpha-neoendorphin (alpha-Neo).
  • To compare the effects of these peptides on hKOR downregulation and internalization in Chinese hamster ovary (CHO) cells.

Main Methods:

  • Stable expression of hKOR in CHO cells.
  • Receptor binding assays.
  • [(35)S]GTPgammaS binding assays to assess G protein stimulation.
  • Measurement of receptor downregulation and internalization following peptide treatment.
  • Experiments conducted with and without serum, and with peptidase inhibitors.

Main Results:

  • Dyn A, Dyn B, and alpha-Neo are potent full agonists of hKOR with comparable efficacy.
  • Dyn A and Dyn B induced significantly greater receptor downregulation (approx. 65%) compared to alpha-Neo (approx. 10%) after 4-h incubation.
  • Alpha-Neo-mediated receptor internalization was also significantly less than that of Dyn A and Dyn B.
  • Serum enhanced alpha-Neo-induced downregulation and internalization, but these effects remained less pronounced than those of Dyn A and Dyn B.

Conclusions:

  • Endogenous dynorphin peptides differentially regulate KOR activity and adaptation despite similar receptor activation efficacy.
  • Peptide stability in serum and intrinsic capacity for receptor adaptation contribute to the observed differences.
  • These findings highlight the complex modulation of KOR signaling by its endogenous ligands.