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Blitzkrieg 7
Ligand-gated channels
24
Biochemistry
Graduate
10/16/2010

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Term
How do ligand gated channels sorta work?
Definition
A ligand binds inducing conformational change opening channel
Term
How long does it take for a ligand gated channel to open?
Definition
Like no time at all. milliseconds?
Term
Are ligand gated channels specific to specific ions?
Definition
NO, they let all the stuff just flowwww
Term
Can you get an action potential caused by a ligand gated channel?
Definition
yes, they can depolarize the membrane causing action potential
Term
What do excitatory ligand gated channels do?
Definition
They get horny. Actually...they usually have stuff flow into the cell. This depolarizes and causes action potential
Term
What do inhibitory ligand gated channels do?
Definition
They let K+ out usually, or bring alotta Cl- in. This hyperPOlarizes the membrane, inhibiting action potential.

However, a point he wants us to know here is that Cl- doesn't actually alter the Vm, it somehow decreases membrane resistance--making it harder for the cell to depolarize
Term
What are the two major families of ligand gated channels?
Definition
Cys-loop and glutamate receptors
Term
What are two famous examples of Cys-loop channels and what do they do?
Definition
nicotinic acetylcholine receptor--nonselective cation channel which depolarizes the membrane (and gets attacked in myasthenia gravis); and GABA receptor--brings in Cl-, inhibiting action potential
Term
What does glutamate receptor do?
Definition
It mediates fast synaptic activity in the brain. There are NMDA type and AMPA type. Activated by excitatory neurotransmitter, glutamate.
Term
What is special about the Cys-loop receptor?
Definition
There is this large extracellular loop at the N-terminus that has cysteine bonds.
Term
How are cys loop channels opened?
Definition
each cys-loop receptor has two binding sites for ligand. each must be bound for the thing to open
Term
What type of ions do nicotinic acetylcholine receptors select for, and how?
Definition
they select for cations by having a bunch of negatively charged residues on the outside
Term
Do nicotinic acetylcholine channels get rid of hydration spheres like other types of channels?
Definition
No, the hydration spheres can fit in
Term
How does the nicotinic acetylcholine receptor gate work?
Definition
When the ligands are unbound, there is a hydrophobic region which swings in towards the channel--blocking it. When the ligands are bound, conformational change forces the hydrophobic segments to swing out, opening gate.
Term
Which type of GABA receptor is ligand gated?
Definition
GABA-A
Term
What is GABA?
Definition
gamma-aminobutyric acid (a neurotransmitter)
Term
What does GABA do?
Definition
mediates fast inhibitory transmission in the brain
Term
What do GABA receptors' channels select for, and how do they do this?
Definition
They are for Cl-, and they do this by having positive residues around the pore
Term
How does GABA gate work?
Definition
Same as NAchR
Term
Why are glutamate receptors considered differently from all the cys-loop ones?
Definition
These guys have a very different structure
Term
What is the pore structure of Glutamate receptor channel?
Definition
There is a little P-loop like thing
Term
What are the two types of glutamate receptors and what are they selective for?
Definition
AMPA is selective for Na+ and K+. NMDA is selective for Ca2+
Term
How are glutamate receptors opened?
Definition
glutamate binds. NMDA also requires glycine and it needs to get extracellular Mg+ away (by having hyperdepolarization)
Term
How does this all happen at a synapse?
Definition
Glutamate is released by presynaptic neuron. Receptors are on postsynaptic neuron. they bind AMPA and NMDA glutamate receptors, but only the AMPA open (because Mg+ is bound to the NMDA). The AMPA start depolarizing the cell by letting in Na+ and K+. This depolarization eventually kicks out the Mg+ from the NMDA because the cell is less negative. Then (assuming glycine is also bound) the NMDA ones will open.

Ca2+ now flows into the postsynaptic neuron through the NMDA channels, activating enzymes and producing long-lasting changes in the efficiency of communication between the presynaptic and postsynaptic neuron that are thought to underlie the formation of memories.
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