GABA receptors

Question 1

List the two types of GABA receptors?

Answer 1

1. GABA A - Ionotropic Receptor

2. GABA B - Metabotropic Receptor.

Question 2

What does GABA Stands for?

Answer 2

GAMMA-AMINOBUTYRIC ACID

Question 3

Metabotropic receptor is also known as

Answer 3

G protein coupled receptor

Question 4

Struture of the GABA A receptor, how many alpha, beta and gamma subunits?

Answer 4

2 alpha subunits
2 beta subunits
1 Gamma subunit

Question 5

GABA receptor has how many binding sites?

Answer 5

3 binding sites
1. Benzodiazepines
2. Gaba binding sites
3

Question 6

Between the alpha and the gamma subunit, what binding site is there

Answer 6

Benzo subunit or BZD allosteric site

Question 7

Between the alpha and the beta subunit, what binding site is there

Answer 7

GABA binding site

Question 8

1st mechanism of action GABA activation

Answer 8

Binding of a ligand or drug to the GABA site or benzodiazepines site–> GABA receptor activated

Question 9

2nd mechanism of action of GABA activation

Answer 9

Due to the binding, the central chloride port opens up and cause an INFLUX OF CHLORIDE IONS

Question 10

what does the influx of Chloride ions causes in GABA? how??

Answer 10

inhibition of the neuro, by creating a state of HYPERPOLARISATION

Question 11

Drugs acting on GABA receptors

Answer 11

GABA - endogenous agonist
Positive allosteric modulators
Negative allosteric modulators

Question 12

What is an endogenous agonist?

Answer 12

an endogenous agonist for a particular receptor is a compound naturally produced by the body which binds to and activates that receptor.

Question 13

Where does the positive allosteric modulators bind to ? Do they cause the same events in the receptor?

Answer 13

Benzodiazepines binding site; yes

Question 14

Classes of Positive Allosteric Modulators (PAM)

Answer 14

1. Benzodiazepines
2. Barbiturates (thiopental)
3. Muscle relaxants
4. Alcohol
5. Propofol and ETOMIDATE

Question 15

Examples Negative allosteric modulators

Answer 15

FLUMAZENIL

Question 16

What is Flumazenil used for?

Answer 16

Benzodiazepines OVERDOSE’

Reveral of anesthesia

Question 17

Effects of Activation of GABA receptors

Answer 17

Anxiolytics
Anticonvulsant
Sedative
Amnesic
Muscle relaxation