GABA neurotransmisson

Question 1

What happens to the membrane when GABA is activated

Answer 1

Activation of GABA receptors causes hyperpolarisation of the membrane

Allowing Cl- to enter the cell

Question 2

What are the 2 types of GABA receptors?

Answer 2

GABA A = LIGAND GATED ION CHANNEL

GABA B = 7TM GPCR

Question 3

GABA synthesis

Answer 3

alpha- ketoglutarate =>
Glutamate =>
GABA

Question 4

Features or the GABA A RECEPTOR

Answer 4

Need 5 subunits (pentameric) =
2 alpha + 2 beta subunits will be Receptor for GABA

Question 5

Where does GABA bind at the GABA A RECEPTOR

Answer 5

At interface between BETA (+ principle) and alpha (- complementary) subunits

Question 6

Name the GABA A RECEPTOR ligands
6 groups

Answer 6

Bicuculline
Benzodiazepines
Barbiturates
Ethanol
General anesthetics
Neurosteroids

Question 7

GABA A ligand

Bicuculline
moa

Answer 7

Competitive antagoinst of GABA A receptors

Question 8

Drug Modulators (agonists) of GABA B RECEPTOR

Answer 8

1. Bacoflen = agonist of GABA B
   = muscle relaxant
2. GHB (fantacy) =
   = treats narcolepsy, alcoholism 🍸

Question 9

In which kind of cells are GABA transports expressed in

Answer 9

Neurons and glial cells

Question 10

Net positive or net negative charge going through the transporter system?

Answer 10

Negative

Question 11

What will happen to GABA is the transporter is inhibited?

Answer 11

Elevate and stimulate GABA neurotransmission

Question 12

Glutaminergic drugs = for mood disorders

Answer 12

Ketamine
Non competitive NMDA Receptor Antagonist that also activates the AMPA Receptor

A drug of abuse
Dissociative anesthetic
Also horse tranquiliser

Question 13

Example of a GAT1 inhibitor (GABA transporter)

Answer 13

Tiagabine