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Ligand-Gated Ion Channels Overview

Jul 7, 2025

Overview

This lecture explains ligand-gated ion channels, their role in fast cellular signaling, their mechanism, and how they differ from other ion channel types.

Types of Membrane Receptors

  • Major membrane receptor types: ligand-gated ion channels, G protein-coupled receptors, enzyme-linked receptors.
  • Focus is on ligand-gated ion channels (also called ion channel linked receptors).

Ligand-Gated Ion Channels: Structure & Function

  • Ligand-gated ion channels are transmembrane proteins that open or close in response to ligand binding.
  • Commonly found in electrically excitable cells like neurons for rapid signal response.
  • Channel is closed until a specific ligand binds to a complementary site ("lock and key" or "induced fit" model).
  • Ligand binding causes a conformational change, opening the channel for ions to move.
  • Binding occurs at an allosteric site, often away from the channel pore itself.

Mechanism & Effects

  • Opening allows ions (like K⁺, Na⁺, Cl⁻, Ca²⁺) to flow through, changing the cell’s electrical properties.
  • Converts an extracellular ligand signal into an intracellular electrical signal.
  • Multiple channels can open simultaneously, amplifying the effect.

Binding Site Details

  • The allosteric binding site is typically on the extracellular side; intracellular binding sites are rare.
  • Some channels have multiple allosteric binding sites for ligands.

Comparison with Other Ion Channels

  • Ligand-gated ion channels are distinct from voltage-gated channels (respond to membrane potential changes).
  • They are also different from stretch-activated ion channels (respond to membrane deformation).

Key Terms & Definitions

  • Ligand-gated ion channel — A transmembrane channel that opens or closes when a ligand binds to it.
  • Ligand — A chemical messenger that binds to a receptor.
  • Allosteric site — A binding site on a protein, separate from the active site, that regulates its function.
  • Voltage-gated ion channel — Opens or closes in response to changes in membrane potential.
  • Stretch-activated ion channel — Opens or closes in response to mechanical deformation of the cell membrane.

Action Items / Next Steps

  • Review the differences between ligand-gated, voltage-gated, and stretch-activated ion channels.
  • Consider examples of ligand-gated ion channels and their physiological roles, especially in neurons.