无感受性TRP通道作为几个抗真菌药物的分子标
Shota Okabe1, Kenji Takahashi1,2, Miho Hashimoto2
1Department of Veterinary Pharmacology, Faculty of Agriculture, Tottori University, Tottori, Japan.
Fundamental & clinical pharmacology
|October 17, 2024
概括
局部抗真菌药物可以通过激活TRPA1和TRPV1通道引起疼痛. 这项研究表明,特定的抗真菌剂直接刺激这些恶感通道,建议在使用时谨慎使用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 神经科学是一个神经科学.
- 皮肤病学 皮肤病学
背景情况:
- 局部抗真菌药可以引起疼痛和刺激.
- 暂时受体潜在 (TRP) 通道,TRPA1和TRPV1,参与感知刺激物.
研究的目的:
- 研究可感性TRP通道在局部抗真菌药物引起的疼痛中的作用.
- 评估各种局部抗真菌剂对TRPA1和TRPV1通道的激活.
主要方法:
- 在表达TRP通道的细胞中评估细胞内度和膜电流.
- 利用异质表达细胞和孤立的小鼠感官神经元.
- 测试了五个不同类别的九种局部抗真菌药物.
主要成果:
- 所有测试的抗真菌药物都增加了TRPA1表达细胞中的细胞内,其中一些显示TRPA1特异性.
- 克洛特里马和凯托可纳激活了TRPA1和TRPV1通道.
- 利拉纳夫和可纳对感觉神经元的影响被TRPA1和/或TRPV1抑制剂或遗传缺失所阻断.
结论:
- 局部抗真菌药物引起的疼痛和刺激与TRPA1和TRPV1通道的激活有关.
- 局部抗真菌药物的临床使用可能需要谨慎,因为这些疼痛感应通道可能会被激活.
相关概念视频
Targets for Drug Action: Overview
6.1K
Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
6.1K
Mechanically-gated Ion Channels
6.3K
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...
6.3K
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
151
Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy. SP binds and activates...
151
Ligand-Gated Ion Channel Receptor: Gating Mechanism
2.1K
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...
2.1K
Enzyme-linked Receptors
77.5K
Enzyme-linked receptors are proteins that act as both receptor and enzyme, activating multiple intracellular signals. This is a large group of receptors that include the receptor tyrosine kinase (RTK) family. Many growth factors and hormones bind to and activate the RTKs.
Neurotrophin (NT) receptors are a family of RTKs, including trkA, trkB, and trkC (tropomyosin-related kinase) receptors. TrkA is specific for nerve growth factor (NGF), neurotrophin-6, and neurotrophin-7. TrkB binds...
Neurotrophin (NT) receptors are a family of RTKs, including trkA, trkB, and trkC (tropomyosin-related kinase) receptors. TrkA is specific for nerve growth factor (NGF), neurotrophin-6, and neurotrophin-7. TrkB binds...
77.5K
Ligand-gated Ion Channels
12.2K
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...
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...
12.2K


