PH2113 - Neuropharmacology 2 Flashcards

1
Q

What is the function of the white matter?

A

Communicating neurones

- myelinated axons

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2
Q

What are the four lobes of the brain?

A

Parietal
Frontal
Occipital
Temporal

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3
Q

What is a gyrus and a sulcus?

A

A gyrus is a prominent rounded elevation - “folds” of brain tissue that form the cerebral hemisphere

Gyri are separated by sulci, which are the grooves or furrows on the surface of the cerebrum - these are the areas between the gyri

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4
Q

What are the two hemispheres of the brain called?

A

Left and right hemispheres

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5
Q

What are the four steps to the transmission of an electrical impulse?

A
Depolarisation to threshold
Activation of sodium channels
- rapid depolarisation
- more positive inside
Inactivation of sodium channels and activation of potassium channels
- membrane potential rectified
Return to normal permeability and resting state
- leak channels
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6
Q

What happens to sodium channels in the membrane of a neurone when the threshold membrane potential is reached?

A

Sodium channels are sensitive to voltage and open when threshold membrane potential is reached

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7
Q

What happens when sodium channels open in an axon?

A

More sodium channels open
Sodium channels behind the action potential become inactive
Action potential can only move in one direction

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8
Q

What is saltatory conduction?

A

The propagation of action potentials along myelinated axons from one node of Ranvier to the next node, increasing the conduction velocity of action potentials

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9
Q

What is neurotransmission?

A

Process of sending signals from nerve to nerve across a synapse

  • membrane depolarisation opens voltage gated calcium channels
  • calcium influx triggers vesicles to move to the pre-synaptic membrane
  • vesicles fuse with the membrane and release their content into the synapse
  • transmitters diffuse across the synaptic cleft
  • transmitter binds to receptors on the post-synaptic membrane
  • may also bind receptors at pre-synaptic neurone to affect release
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10
Q

Give examples of two receptors that neurotransmitter can bind to

A

Ligand-gated ion channel receptors

G-protein linked receptors

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11
Q

What factors are all defined by the receptor’s structure?

A
Ligand binding site
Antagonist binding sites
Ion channel domains
Recognition sites for extra- and intra-cellular modulators
Sites of contact for regulatory proteins
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12
Q

What are the three units that make up the sodium channel?

A
alpha unit
- forms the pore in the membrane channel
beta-1 unit
- regulatory
- transmembrane
beta-2 unit
- regulatory
- on extracellular side
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13
Q

What is the role of the voltage-gated sodium channel?

A

Rising phase of the action potential

  • voltage dependent gating
  • depolarisation
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14
Q

How many subtypes are there of the voltage-gated sodium channel?

A

9 functional members of the family

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15
Q

Why are there different subtypes of voltage-gated sodium channel?

A

Tissue specific

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16
Q

What is the structure of the voltage-gated sodium channel?

A

6 transmembrane spanning domains

  • different functions
  • S5 and S6 present on all subunits
17
Q

How is the voltage-gated sodium channel inactivated?

A

Hinged-lid mechanism

- intracellular loop containing domains III and IV of the channel is depicted as forming a hinged lid

18
Q

How do local anaesthetics work?

A

Reversible voltage-gated sodium channel blockade

  • lipophilicity important for permeation
  • charge is important for block
  • mode of entry depends on the drug

Block action potential in all sensory, motor and autonomic fibres

  • cannot transmit pain
  • voltage-gated sodium channels 1.7 and 1.8 are targets in pain
19
Q

What might a large topical doses of local anaesthetic cause?

A

Systemic toxicity

20
Q

Give four classes of drugs that target the voltage-gated sodium channel

A

Local anaesthetics
Antiepileptics
Neuropathic pain
Anti-arrhythmics