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Related Concept Videos

Opioid Receptors: Overview01:22

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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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The Two-State Receptor Model01:29

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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.
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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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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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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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The delta opioid receptor tool box.

Ana Vicente-Sanchez1, Laura Segura1, Amynah A Pradhan1

  • 1Department of Psychiatry, University of Illinois at Chicago, United States.

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|June 29, 2016
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Summary

This review details tools for studying the delta opioid receptor (DOR), crucial for treating pain and emotional disorders. It guides researchers on assay, ligand, detection, behavioral, and genetic methods for DOR research.

Keywords:
G protein-coupled receptorcell linesmutant micepain

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Area of Science:

  • Neuroscience
  • Pharmacology

Background:

  • The delta opioid receptor (DOR) is a key target for managing chronic pain and emotional disorders.
  • Developing effective therapeutic strategies necessitates a deep understanding of DOR molecular and functional properties.

Purpose of the Study:

  • To provide a comprehensive overview of available tools for delta opioid receptor research.
  • To guide researchers in selecting and utilizing appropriate methods for studying DOR.
  • To highlight the applications and limitations of various DOR research tools.

Main Methods:

  • Review of cell-based assays for DOR.
  • Analysis of peptide and non-peptide DOR ligands.
  • Examination of techniques for detecting DOR in fixed tissues.
  • Description of behavioral assays for in vivo DOR agonist effects.
  • Characterization of genetically modified mouse models for DOR studies.

Main Results:

  • Summarizes diverse tools including cell assays, ligands, tissue detection methods, behavioral tests, and genetically modified mice.
  • Discusses the utility and constraints associated with each research approach.
  • Highlights specific in vivo effects like locomotor stimulation and convulsions induced by DOR agonists.

Conclusions:

  • This review serves as a guideline for employing various tools to investigate delta opioid receptor physiology.
  • Effective utilization of these methods will enhance the understanding of DOR function.
  • Informed tool selection is critical for advancing DOR-targeted therapeutics.