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Related Concept Videos

Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

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Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
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Ion Channels01:19

Ion Channels

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The movement of ions like sodium, potassium, and calcium into and out of the cell is essential to maintain the electrochemical gradient in living cells. The ion channels—a class of membrane transport proteins—help maintain this ionic gradient for the smooth functioning of physiological activities such as maintaining cell size and volume, conducting nerve impulses, and gas and nutrient exchange.
Ion channels are specialized integral membrane proteins on the plasma membrane that allow...
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Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

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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...
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Ligand Binding Sites02:40

Ligand Binding Sites

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Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
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Metal-Ligand Bonds02:51

Metal-Ligand Bonds

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The hemoglobin in the blood, the chlorophyll in green plants, vitamin B-12, and the catalyst used in the manufacture of polyethylene all contain coordination compounds. Ions of the metals, especially the transition metals, are likely to form complexes.
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Ligand Binding and Linkage00:49

Ligand Binding and Linkage

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Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence...
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Tobacco Hornworm as an Insect Model System for Cannabinoid Pre-clinical Studies
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Cannabinoid Ligands Targeting TRP Channels.

Chanté Muller1, Paula Morales1, Patricia H Reggio1

  • 1Department of Chemistry and Biochemistry, University of North Carolina at Greensboro, Greensboro, NC, United States.

Frontiers in Molecular Neuroscience
|January 31, 2019
PubMed
Summary

Cannabinoids modulate specific Transient Receptor Potential (TRP) channels, including TRPV, TRPA, and TRPM subfamilies. This interaction offers potential therapeutic avenues for conditions linked to TRP channel dysfunction.

Keywords:
TRP channelsTRPA1TRPM8TRPV1cannabidiolcannabinoids

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Area of Science:

  • Molecular Biology
  • Neuroscience
  • Pharmacology

Background:

  • Transient Receptor Potential (TRP) channels are crucial for sensing stimuli and are implicated in various physiological processes and diseases.
  • Dysfunction of TRP channels is linked to conditions such as neuropathic pain, inflammation, and respiratory disorders.
  • Cannabinoids, including endogenous, plant-derived, and synthetic compounds, have emerged as modulators of specific TRP channel subfamilies.

Purpose of the Study:

  • To review and classify cannabinoid ligands that modulate TRP channels.
  • To explore the therapeutic potential of these cannabinoid-TRP channel interactions.

Main Methods:

  • Literature review of studies investigating cannabinoid interactions with TRP channels.
  • Classification of identified cannabinoid ligands based on the TRP channel subfamilies they modulate (TRPV, TRPA, TRPM).
  • Analysis of reported effects of specific cannabinoids, such as anandamide, N-arachidonyl dopamine, Δ9-tetrahydrocannabinol, and WIN55,212-2, on TRP channels.

Main Results:

  • Six TRP channels—TRPV1, TRPV2, TRPV3, TRPV4, TRPA1, and TRPM8—are reported to be modulated by cannabinoids.
  • Endocannabinoids like anandamide (AEA) and N-arachidonyl dopamine (NADA) interact with TRPV1 and TRPM8.
  • Phytocannabinoids like Δ9-tetrahydrocannabinol (Δ9-THC) show varied potency across TRPV2, TRPV3, TRPV4, TRPA1, and TRPM8, while synthetic cannabinoids like WIN55,212-2 can modulate TRPA1 and TRPV1.

Conclusions:

  • TRP channels, particularly TRPV, TRPA, and TRPM subfamilies, represent a significant target for cannabinoid action, potentially acting as 'ionotropic cannabinoid receptors'.
  • The diverse interactions between cannabinoids and TRP channels highlight their potential as therapeutic targets for pain, inflammation, and other disorders.
  • Further research into these interactions could lead to novel therapeutic strategies leveraging cannabinoid-TRP channel modulation.