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October, 2006
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Ligand-Gated Ion Channels: A subclass of ion channels that open or close in response to the binding of specific Ligands.

Ion Channels

JoVE 10722

Ion channels maintain the membrane potential of a cell. For most cells, especially excitable ones, the inside has a more negative charge than the outside of the cell, due to a greater number of negative ions than positive ions. For excitable cells, like firing neurons, contracting muscle cells, or sensory touch cells, the membrane potential must be able to change rapidly moving from a negative membrane potential to one that is more positive. To achieve this, cells rely on two types of ion channels: ligand-gated and voltage-gated. Ligand-gated ion channels, also called ionotropic receptors, are transmembrane proteins that form a channel but which also have a binding site. When a ligand binds to the surface, it opens the ion channel. Common ionotropic receptors include the NMDA, kainite, and AMPA glutamate receptors and the nicotinic acetylcholine receptors. When a ligand, like glutamate or acetylcholine, binds to its receptor it allows the influx of sodium (Na+) and calcium (Ca++) ions into the cells. The positive ions, or cations, follow down their electrochemical gradient, moving from the more positive extracellular surface to the less positive (more negative) intracellular surface. This changes the membrane potential near the receptor, which can then activate nearby voltage gated ion channels to propagate the change in membrane potential throughout the cell

 Core: Cell Signaling

Cell-surface Signaling

JoVE 10877

Hormones—or any molecule that binds to a receptor, known as a ligand—that are lipid-insoluble (water-soluble) are not able to diffuse across the cell membrane. In order to be able to affect a cell without entering it, these hormones bind to receptors on the cell membrane. When a first messenger, a hormone, binds to a receptor, a signal cascade is set off, causing second messengers, proteins inside the cell, to become activated, resulting in downstream effects. Cell membrane receptors have three portions: an external ligand-binding domain, a transmembrane domain, and an internal domain. There are three categories of cell membrane receptors based on the consistency of the structure and function of these domains within each category. One category is ligand-gated ion channels which, when bound to a ligand, undergo a conformational change, allowing ions through a channel formed by the transmembrane portion of the receptor. A second category is G-proteins-coupled receptors which have a distinct structure with seven transmembrane domains. Binding of the external domain to a ligand causes the alpha subunit, one of three subunits attached to the internal portion of the receptor, to disassociate from the receptor and create a cellular response. The third category of receptors, the enzyme-linked receptor—also called catalytic receptor

 Core: Endocrine System

Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels

1Department of Physiology, David Geffen School of Medicine, University of California, Los Angeles, 2Department of Anesthesiology, David Geffen School of Medicine, University of California, Los Angeles, 3Department of Anesthesiology, Medicine and Physiology, David Geffen School of Medicine, University of California, Los Angeles

JoVE 1178

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