Related Experiment Video

Updated: Dec 18, 2025

Preparation of Acute Brain Slices Using an Optimized N-Methyl-D-glucamine Protective Recovery Method
10:53

Preparation of Acute Brain Slices Using an Optimized N-Methyl-D-glucamine Protective Recovery Method

Published on: February 26, 2018

48.1K

Opioid Receptor Regulation of Neuronal Voltage-Gated Calcium Channels

Norbert Weiss1,2, Gerald W Zamponi3

  • 1Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Prague, Czech Republic.

Cellular and Molecular Neurobiology
|June 10, 2020
PubMed

Insights

Neuronal voltage-gated calcium channels are regulated by opioid and nociceptin receptors via G-protein coupled receptors (GPCRs). This regulation is crucial for neuronal function and offers potential for novel pain therapeutics.

Area of Science:

  • Neuroscience
  • Molecular Biology
  • Pharmacology

Background:

  • Neuronal voltage-gated calcium channels are essential for neurotransmitter release.
  • G-protein coupled receptors (GPCRs), including opioid and nociceptin receptors, modulate channel activity.
  • GPCRs physically interact with calcium channels, affecting their function and cell surface expression.

Purpose of the Study:

  • To review the mechanisms of calcium channel regulation by opioid and nociceptin receptors.
  • To highlight the role of this regulation in neuronal function and disease.
  • To discuss novel receptor modulators as potential pain treatments.

Main Methods:

  • Literature review of mechanisms regulating neuronal calcium channels.
  • Analysis of GPCR and opioid/nociceptin receptor interactions with calcium channels.
  • Examination of recent studies on novel receptor modulators.

Main Results:

  • Opioid and nociceptin receptors fine-tune synaptic activity by regulating calcium channels.
  • Dysregulation of these pathways is implicated in various diseases.
  • Novel μ-opioid receptor/nociceptin receptor modulators show therapeutic promise.

Conclusions:

  • Regulation of neuronal calcium channels by opioid and nociceptin receptors is a key mechanism in synaptic plasticity.
  • Understanding these interactions is vital for developing targeted pain therapies.
  • Emerging drug candidates targeting these receptors may offer new avenues for pain management.
Keywords:
G-protein coupled receptorsMu opioid receptorNociception opioid receptorVoltage-gated calcium channels

More Related Videos

Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis07:48

Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis

Published on: July 3, 2015

9.1K
Visualizing Shifts on Neuron-Glia Circuit with the Calcium Imaging Technique11:41

Visualizing Shifts on Neuron-Glia Circuit with the Calcium Imaging Technique

Published on: April 8, 2022

4.9K

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,...
3.6K
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
3.6K
Analgesia and Pain Management01:25

Analgesia and Pain Management

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...
1.3K
The Role of Ion Channels in Neuronal Computation01:19

The Role of Ion Channels in Neuronal Computation

A postsynaptic neuron usually receives numerous impulses from several other presynaptic neurons. The axon hillock of the postsynaptic neuron integrates all these signals and determines the likelihood of firing an action potential.
Sometimes a single EPSP is strong enough to induce an action potential in the postsynaptic neuron. However, multiple presynaptic inputs must often create EPSPs around the same time for the postsynaptic neuron to be sufficiently depolarized to fire an action potential....
3.5K
Feedback Regulation of Calcium Concentration01:27

Feedback Regulation of Calcium Concentration

Calcium is an essential signaling molecule required for various cellular functions. Calcium pumps and ion channels on cell and organellar membranes, such as those on the endoplasmic reticulum (ER), regulate calcium concentrations inside the cell. They remain closed, keeping the cytosolic calcium levels low at a resting state.
Various transmembrane receptors, such as G protein-coupled receptors (GPCRs), elicit a response to extracellular signals by increasing cytosolic calcium. Activated GPCRs...
3.8K
Voltage-gated Ion Channels01:26

Voltage-gated Ion Channels

Voltage-gated ion channels are transmembrane proteins that open and close in response to changes in the membrane potential. They are present on the membranes of all electrically excitable cells such as neurons, heart, and muscle cells.
Generally, all voltage-gated ion channels have a 'voltage-sensing domain' that spans the lipid bilayer. The charged residues in the sensor move in response to the membrane potential changes that open the channel allowing ions movement. There are several...
10.0K