Ligand gated ion channels and GPCR's

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What is a receptor?

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  • Causes a response via cellular change
  • Main target for a drug
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What is another name for ligand gated ion channels?

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Intropic receptors

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20 Terms

1
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What is a receptor?

  • 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?

Seconds

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What is a G-protein coupled receptor made up of?

  • 7-transmembrane domains
  • Extracellular N-terminus
  • Intracellular C-terminus
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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
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What are the different Ga subtypes?

GaS (stimulate), Gai (inhibit), GaQ, Ga12

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What are effectors?

Ion channels ad enzymes

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What are 2nd messengers?

Ions, intracellular

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What are some roles of GPCR?

Vascular tone, airway constriction and relaxation, heart contractility, acid secretion, mood, pathogen defense.

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How does vascular tone relate to GPCR?

  • Arteries/arterioles contain smooth muscle
  • Constriction reduces diameter whereas relaxation increases diameter of the vessel.
  • This impacts blood pressure.
  • Tone is controlled by: circulating factors (e.g. adrenaline), symp and parasymp nervous system, paracrine factors.