Gaba - continued

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Agonist at the GabaA receptor
Muscimol
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Antagonists at the GabaA recetpor
bicuculline, binds to the GABA binding site. Picrotoxin blocks the chloride channel. These cause convulsions
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GABAa modulatory drugs
Benzodiazapines bind at the site of interface of a and y subunits. Barbituates, neurosteroids, ethanol, anaestheitcs
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What are GabaB receptors coupled to?
Gi - to inhibit adenyl cyclase. and coupled to ion channels via the B/y subunits.
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What is the pre-synaptic effect
Long lasting inhibition of vg Ca2+ channels, decreasign transmitter release.
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Where are they found, presynaptically?
On glutamate and GABA containing terminals
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Post synaptic inhibition effect
increased opening of K+ channels to reduce firing of action potentials.
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Where is glycine used as an inhibitory transmitter
spinal cord, brain stem, retina, auditory systems, sensory systems.
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How is glycine synthesised
serine is catalysed to glycine by serine hydroxymethyl transferase.
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How does glycine get in to vesicles
H+ dependant vesicular inhibitory amino acid transporter
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How is glycine reuptaken
by glia - terminaates the action. By presynpatic transporter - reused. Driven by Na+ and Cl- gradients.
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What is the Glycine receptor like
A pentameric recetpor with 4 alpha subunits, and one type of B subunit. Glycine binds an an A subunit. Each subunit has 4 tmds
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Name of a glycine receptor antagonist
Strychnine.
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How does picrotoxin inhibit
non-competatively
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What happens if there is a mutation in human glycine receptor
Hyperekplexia. 100 fold decrease in glycine affinity, increased muscle tone and startle reflex
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Card 2

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Antagonists at the GabaA recetpor

Back

bicuculline, binds to the GABA binding site. Picrotoxin blocks the chloride channel. These cause convulsions

Card 3

Front

GABAa modulatory drugs

Back

Preview of the front of card 3

Card 4

Front

What are GabaB receptors coupled to?

Back

Preview of the front of card 4

Card 5

Front

What is the pre-synaptic effect

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