Related Experiment Video
Updated: Jun 4, 2026
12:09
Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
Published on: December 31, 2013
Synthetic modulators of TRP channel activity
Christian Harteneck1, Chihab Klose, Dietmar Krautwurst
1Institute for Pharmacology and Toxicology, Interfaculty Center of Pharmacogenomics and Pharmaceutical Research (ICEPHA), Eberhard-Karls-University, Tübingen, Germany. Christian.Harteneck@uni-tuebingen.de
Advances in Experimental Medicine and Biology
|February 4, 2011
Summary
Transient Receptor Potential (TRP) channels are crucial for sensing stimuli like heat and pain. While TRPV1-targeting drugs are advancing, research continues for selective modulators of other TRP channels due to their diverse functions.
Area of Science:
- Physiology
- Pharmacology
- Molecular Biology
Background:
- Transient Receptor Potential (TRP) channels, comprising 27 members in 6 families, are vital for cellular functions including thermosensation, pain, and chemosensation.
- Naturally occurring compounds activating TRPV1, TRPM8, and TRPA1 channels often function as defense mechanisms, highlighting their role in pain and inflammation.
Purpose of the Study:
- To provide an overview of available broad-range blockers and the emerging selective compounds targeting TRP channels.
- To discuss the challenges and progress in developing selective drugs for TRP channels beyond TRPV1.
Main Methods:
- Literature review of existing TRP channel modulators.
- Analysis of the development landscape for TRPV1-selective ligands versus other TRP channels.
Main Results:
- The discovery of TRPV1's role in nociception spurred the development of selective ligands.
- Limited understanding of other TRP channels' physiological roles has hindered the development of selective drugs, resulting in mostly non-selective blockers.
Conclusions:
- There is an ongoing need for novel, selective natural and synthetic ligands and modulators for various TRP channels.
- Current therapeutic strategies largely rely on broad-range blockers due to the lack of selectivity for many TRP channels.
Related Concept Videos
01:30Ligand-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...
01:12Mechanically-gated Ion Channels
Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
01:12Mechanically-gated Ion Channels
Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
01:22Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
The direct-acting...
01:19Ligand-gated Ion Channels
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 include the...
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 include the...
01:19Ligand-gated Ion Channels
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 include the...
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 include the...