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3922 > 7 - LGIC > Flashcards

7 - LGIC Flashcards

1
Q

What are the two excitatory LGIC

A

nAChR

5-HT3R

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2
Q

What are two inhibitory LGIC

A

GABAAR

Strychnine-sensitive glycine receptors

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3
Q

What are two excitatory ionotropic glutamate receptors

A

AMPA
Kainate
NMDA

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4
Q

What confers ion selectivity of LGICs

A

M2 pore lining helices

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5
Q

What keeps LGICs in a closed conformation

A

a helices bent towards centre of pore leading to a narrow region too narrow and hydrophobic to allow ion passage

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6
Q

How does the LGIC pore open

A

Via rotation or tilting of the pore lining helices

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7
Q

What does bicuculline do

A

Competitive antagonist of most GABAAR

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8
Q

What do benzodiazepines do

A

Enhance actions of GABA

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9
Q

What do barbituates do

A

Act alone or enhance actions of GABA

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10
Q

What are BZ selective for GABAAR

A

a1, a2, a3, a5 and Y

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11
Q

What do PB act on

A

GABAAR

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12
Q

What is crucial to BZ binding

A

Histidine which is not present in a4 and a6

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13
Q

What do benzodiazepines cause (3)

A

Sedation
Muscle relaxation
Anxiolysis

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14
Q

What subunit mediates sedative action

A

a1

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15
Q

What subunit mediates anxiolysis action

A

a2

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16
Q

What subunits mediate muscle relaxation

A

a2 and a3

17
Q

What subunits mediate impaired motor coordination

A

a1 and a3

18
Q

What is the MOA of ethanol

A

Enhance actions of GABA
Prolongs the open time of the channel
Bind within the transmembrane domain

19
Q

What is the MOA of GA

A

Enhance the actions of GABA
Directly stimulate receptors at high concentration
Bind at the interface between a and b subunits within the transmembrane region of the channel

20
Q

What is the MOA of neurosteroids

A

Promote channel opening

Receptors containing y subunit are most sensitive

21
Q

Glycine and strychnine bind at the subunit interface true or false

A

True

22
Q

Where does ivermectin bind

A

Within the membrane of glyR

23
Q

Where does picrotoxin bind

A

Within pore of the channel

24
Q

Which GlyR has lower affinity for picrotoxins

A

Heteromeric GlyR

25
Q

What are some 5HT3 receptor antagonists

A

Alosetron

Ondansetron

26
Q

Where is ondansetron likely to bind

A

5HT3 binding site at the interface between subunits

27
Q

AMPA receptors are fast or slow

A

Fast

28
Q

NMDA receptors are fast or slow

A

Slow

29
Q

Which of AMPA or NMDA allow for both NA and Ca permeation

A

NMDA

30
Q

What elicits a voltage dependent block of NMDA receptors

A

Mg

31
Q

What does glutamate binding do to the NMDA receptor

A

Pushes the gate apart to allow channel opening

32
Q

What is the selectivity filter of the NMDA pore

A

Residues in TM2 control cation permeability - RNA editing

3922 (19 decks)

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