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Ligand-gated ion channels

Ligand-gated ion channels, also known as ionotropic receptors, are a group of transmembrane ion channels that open or close in response to the binding of a chemical messenger, or "ligand". These ligands can include neurotransmitters such as glutamate, GABA, acetylcholine, and glycine, among others.

Upon ligand binding, the channels undergo a conformational change that allows for the selective passage of ions such as sodium, potassium, calcium, and/or chloride across the cell membrane. This changes the voltage across the cell membrane and can either stimulate or inhibit the cell's action potential, depending on the specific type of channel and ion.

These channels play a key role in the fast synaptic transmission of electrical signals in the nervous system, allowing for rapid responses to changes in the environment. They are also found in other types of cells and tissues and play important roles in processes such as muscle contraction and sensory perception.

Ligand-gated ion channels consist of multiple subunits that together form a pore through the cell membrane. Each subunit has a site that can bind a ligand, and the binding of the ligand to these sites triggers the opening of the channel.

Defects in the function of these channels can lead to numerous diseases, such as epilepsy, autoimmune diseases, and certain genetic disorders. Understanding the function of these channels and how they can be manipulated by drugs is therefore a major area of biomedical research.

Ligand-gated ion channels are typically divided into three main types, based on the neurotransmitter that binds to them:

  1. Nicotinic Acetylcholine Receptors (nAChRs): These channels open when they bind the neurotransmitter acetylcholine or nicotine. They are found in many places in the body, including the neuromuscular junction where motor neurons connect with muscle cells, and in the central nervous system. These channels typically allow the passage of sodium and potassium ions, leading to an excitatory response.

  2. Ionotropic Glutamate Receptors (iGluRs): These channels open when they bind the neurotransmitter glutamate. They are found primarily in the central nervous system and are involved in most of the excitatory neurotransmission in the brain. There are three main types of iGluRs: AMPA receptors, NMDA receptors, and kainate receptors. They typically allow the passage of sodium, potassium, and sometimes calcium ions.

  3. GABA and Glycine Receptors: These channels open when they bind the neurotransmitters GABA (for GABAA receptors) or glycine. They are found in the central nervous system and typically have inhibitory effects because they allow the passage of chloride ions, which usually reduces the likelihood of an action potential.

There are also other types of ligand-gated ion channels that are not classified under these three main types, such as the 5-HT3 receptor, a serotonin-gated ion channel, and the P2X receptor, an ATP-gated ion channel.

Each of these types can be further divided into subtypes based on their structure and function, and different subtypes can be found in different parts of the nervous system and body. These subtypes can have different properties, such as sensitivity to drugs or speed of response.


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