GABA Flashcards

1
Q

BZs modulate__________ but have no effect on

A

GABA binding affinity

Maximal efficacy

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2
Q

What sort of shift does diazepam cause on gaba concentration effect curve

A

Leftwards

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3
Q

Flumazenil binds to

But has

A

Same site as diazepam

No effect on curve

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4
Q

What residue is essential for classical BZs binding?

A

H101

Mutate to R means diazepam won’t bind

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5
Q

A1 involved in

A

Sedation

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6
Q

Selective affinity

A

Higher affinity for receptors containing certain subunits

No compounds found that bind 2+3 but not 1

Compounds may still have same max efficacy

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7
Q

Selective efficacy

A

Affinity for all but only efficacy at 5

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8
Q

NS are subtype specific

A

False

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9
Q

Alfaxalone

A

Enhances GABA action on receptors
Very specific- steroids with similar structure are not anaesthetic
GABAaRs might have binding site

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10
Q

What does NMDAR activation do to NS synthesis?

A

Excessive NMDAR activation turns on NS synthesis to enhance inhibition

Protects from excessive excitation

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