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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...
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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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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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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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Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis
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Published on: July 3, 2015

Current research on opioid receptor function.

Yuan Feng1, Xiaozhou He, Yilin Yang

  • 1Yale University School of Medicine, New Haven, CT, USA.

Current Drug Targets
|December 30, 2011
PubMed
Summary
This summary is machine-generated.

Opioid receptors, particularly the delta-opioid receptor (DOR), offer neuroprotection and cardioprotection. DOR activation enhances neuronal survival against hypoxic/ischemic stress, with potential clinical applications for stroke and heart attack treatment.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Cardiology

Background:

  • Opioid analgesics have a long history, but their receptor mechanisms are not fully understood.
  • Three major opioid receptors (MOR, DOR, KOR) exist, with DOR showing promise in neuroprotection and cardioprotection.
  • Opioid receptors influence diverse functions beyond pain, including homeostasis, cell proliferation, and cardiovascular control.

Purpose of the Study:

  • To review recent research on opioid receptors and their functions.
  • To provide insights into the physiological and pharmacological roles of opioid receptors.
  • To highlight the potential of DOR-mediated protection in clinical settings.

Main Methods:

  • Literature review of recent studies on opioid receptor function.
  • Analysis of research on DOR-mediated neuroprotection and cardioprotection.
  • Examination of signaling pathways involved in opioid receptor activity.

Main Results:

  • DOR activation increases neuronal tolerance to hypoxic/ischemic stress.
  • DOR signaling involves pathways like PKC-ERK-Bcl 2, enhancing survival and antioxidative capacity.
  • Opioid receptors, particularly DOR, demonstrate significant cardioprotective effects involving PKC and KATP channels.

Conclusions:

  • DOR-mediated neuroprotection and cardioprotection hold significant potential for treating stroke and myocardial infarction.
  • Further understanding of the opioid system can lead to novel therapeutic strategies.
  • Opioid receptors play a critical role in physiological and pathophysiological processes beyond pain management.