GABA Flashcards Preview

Molecular Pharmacology > GABA > Flashcards

Flashcards in GABA Deck (10):
1

BZs modulate__________ but have no effect on

GABA binding affinity
Maximal efficacy

2

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

Leftwards

3

Flumazenil binds to

But has

Same site as diazepam
No effect on curve

4

What residue is essential for classical BZs binding?

H101

Mutate to R means diazepam won’t bind

5

A1 involved in

Sedation

6

Selective affinity

Higher affinity for receptors containing certain subunits

No compounds found that bind 2+3 but not 1

Compounds may still have same max efficacy

7

Selective efficacy

Affinity for all but only efficacy at 5

8

NS are subtype specific

False

9

Alfaxalone

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

10

What does NMDAR activation do to NS synthesis?

Excessive NMDAR activation turns on NS synthesis to enhance inhibition

Protects from excessive excitation