CBG32 Flashcards

1
Q

What is nAChR?

A

Nicotonic Ach receptor

major receptor at neuromuscular junction - first ligand gated receptor protein to be purified.

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2
Q

Why was nAChR the first ligand gated receptor to be purified?

A
  1. high concentrations found in great numbers in electroplax organ of eimobrach (electric eel) and teleost
    - 1kg of electrical organ contains over 100mg of
    receptor protein.
  2. sensitivity of nAChR’s to alpha-BTX - a component of cobra venom useful in study to tag AChRs
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3
Q

What is the structure of the nictotine acetylcholine receptor?

A

pentametric
- 5 proteins subunits associated to form a transmembrane channel. 2xalpha 1xdelta 1xlambda 1xbeta
- alpha subunits contain sites that bind ACh
- negatively charge internal portion bears the selectivity filter for Na+ and K+
Each subunit is 55kDa
- 275KDa in total

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4
Q

What happens when ACh binds to alpha subunit

A
causes a conformational change 
pore opens 
Na+ flow in/K+ out down electrochemical gradient
excitatory receptor
membrane deploarisation
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5
Q

What are the 3 functional states of nAChR?

A
  1. resting - closed - no ACh bound.
  2. Activated - open - 2ACh bound - can flicker between open and closed state with ACh bound
  3. Desensitised - ACh still bound but closed
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6
Q

what is gaba?

A

the chief inhibitory neurotransmitter in the mammalian central nervous system. It plays the principal role in reducing neuronal excitability throughout the nervous system.

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7
Q

What is the structure of muscarinic acetylcholine receptor mAChR?

A

460AA
70kDA
7TM receptor
interacts with 6 proteins

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