GABA

Question 1

BZs modulate__________ but have no effect on

Answer 1

GABA binding affinity

Maximal efficacy

Question 2

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

Answer 2

Leftwards

Question 3

Flumazenil binds to

But has

Answer 3

Same site as diazepam

No effect on curve

Question 4

What residue is essential for classical BZs binding?

Answer 4

H101

Mutate to R means diazepam won’t bind

Question 5

A1 involved in

Answer 5

Sedation

Question 6

Selective affinity

Answer 6

Higher affinity for receptors containing certain subunits

No compounds found that bind 2+3 but not 1

Compounds may still have same max efficacy

Question 7

Selective efficacy

Answer 7

Affinity for all but only efficacy at 5

Question 8

NS are subtype specific

Answer 8

False

Question 9

Alfaxalone

Answer 9

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

Question 10

What does NMDAR activation do to NS synthesis?

Answer 10

Excessive NMDAR activation turns on NS synthesis to enhance inhibition

Protects from excessive excitation