- Causes a response via cellular change - Main target for a drug
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What is another name for ligand gated ion channels?
Intropic receptors
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How long does a ligand gated ion channel take to activate?
Milliseconds
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What are the key features of a ligand gated ion channel?
- Form a channel between intracellular and extracellular environment of a cell. - Number of subunits vary between channels - Either activate signally or change excitability of the cell
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What is an example of a ligand gated ion channel?
Nicotinic acetylcholine receptor
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How do nicotinic Ach receptors work?
Agonist binds to the receptor causing Na+ ions to move into the cell and become excited, causing depolarisation.
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how does the GABAa receptor control Cl- flow?
- Activation of GABA via an agonist - Receptor activation increases Cl- movement through ion channel - Cell membrane hyperpolarizes - Result is decreased excitability
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How does the neuromuscular junction work?
Motor nerves from the spinal cord synapse with skeletal muscle fibres, then each branch forms an end plate region on a motor end plate, initiating contraction.
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What are some clinical uses of antagonists?
Tracheal intubation, surgical procedures e.g. abdominal surgery, therapeutic hypothermia.
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How can antagonists treat therapeutic hypothermia?
Cardiac arrest, reduce body temp to 32-34 degrees, improves neurological recovery, prevents shivering. Can only be done after anaesthetic as effects whole body.
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What is another name for a G-protein coupled receptor?
7 transmembrane receptor or metabotropic receptor
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How long does a G-protein coupled receptor take to work?
What are key features of G-protein coupled receptors?
- Largest family of receptors in the body - Highly druggable, almost half of prescription drugs work on them.
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What is the basic mechanism of a G-protein coupled receptor?
1. Agonist binds to 7-TM receptor, initiating signalling 2. Signal stimulates G protein, causing it to move along the membrane 3. Effector is activated or inhibited triggers response