PRG - New Drug Targets2

Question 1

Anti epileptic drugs; Felbamate, Gabapentin and Topirmatee are excitatory or inhibitory?

Answer 1

Excitatory.

Question 2

Anti epileptic drugs; Benzodiazepines, Vigabatrin and Tiagabine are excitatory or inhibitory?

Answer 2

Inhibitory.

Question 3

Which AED works on L-type-lca+?

Answer 3

Gabapentin. Excitatory.

Question 4

Which AED works on GABA-R?

Answer 4

Benzodiazepines. Inhibitory.

Question 5

Which AED works on GABA-RUI?

Answer 5

Tiagabine. Inhibitory.

Question 6

Which AED works on NMDA?

Answer 6

Felbamate. Excitatory.

Question 7

Which AED works on AMPA?

Answer 7

Topirmate. Excitatory.

Question 8

Which AED works on GABA-T?

Answer 8

Vigabatrin. Inhibitory.

Question 9

What converts Angiotensinogen into Angiotensin I?

Answer 9

Renin.

Question 10

What converts Angiotensin I to Angiotensin II?

Answer 10

ACE.

Question 11

What receptors does Angiotensin II work on?

Answer 11

AT1 and AT2 receptors.

Question 12

What do aminopeptidase A and N enzymes do respectively?

Answer 12

Convert Angiotensin II to III and then IV, respectively.

Question 13

Where is angiotensinogen made? And how many amino acids? Which of the amino acids are important for the renin angiotensin system?

Answer 13

Liver. 452. Only the terminal 14 amino acids are important for the renin angiotensin system.

Question 14

Where is renin made?

Answer 14

Kidney.

Question 15

What is Bothrops jararaca? How does it work?

Answer 15

Venom. Potent inhibitor of ACE and potentiates hypotensive effect of circulating bradykinin.

Question 16

Systemic effects of Bothrops jararaca venom?

Answer 16

Spontaneous haemorrhage (cerebral**), disseminated intravascular coagulation, and cardiovascular shock secondary to hypovolemia and vasodilation.

Question 17

Name the peptide from Bothrops jararaca venom that acts as a potent, selective ACE inhibitor.

Answer 17

Teprotide.

Question 18

What do the substrates for ACE require? (4 things)

Answer 18

1. Free carboxyl group on the C-terminal
2. Proline is NOT present in penultimate position to C-terminal
3. Hydrophobic amino acid is present at the antepenultimate position to the C-terminal
4. Gly, Ala, Val, Leu, Ile, Pro, Phe, Met and Trp

Question 19

What is the outcome of the presence of proline in the penultimate position?

Answer 19

Renders peptide resistant to ACE.

Question 20

Like how angiotensin II works on AT1 and AT2 receptors, what does angiotensin IV work on?

Answer 20

AT4 receptors

Question 21

AT4 receptors are also known as?

Answer 21

(IRAP)