PRG - New Drug Targets2 Flashcards Preview

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Flashcards in PRG - New Drug Targets2 Deck (21):
1

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

Excitatory.

2

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

Inhibitory.

3

Which AED works on L-type-lca+?

Gabapentin. Excitatory.

4

Which AED works on GABA-R?

Benzodiazepines. Inhibitory.

5

Which AED works on GABA-RUI?

Tiagabine. Inhibitory.

6

Which AED works on NMDA?

Felbamate. Excitatory.

7

Which AED works on AMPA?

Topirmate. Excitatory.

8

Which AED works on GABA-T?

Vigabatrin. Inhibitory.

9

What converts Angiotensinogen into Angiotensin I?

Renin.

10

What converts Angiotensin I to Angiotensin II?

ACE.

11

What receptors does Angiotensin II work on?

AT1 and AT2 receptors.

12

What do aminopeptidase A and N enzymes do respectively?

Convert Angiotensin II to III and then IV, respectively.

13

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

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

14

Where is renin made?

Kidney.

15

What is Bothrops jararaca? How does it work?

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

16

Systemic effects of Bothrops jararaca venom?

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

17

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

Teprotide.

18

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

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

19

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

Renders peptide resistant to ACE.

20

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

AT4 receptors

21

AT4 receptors are also known as?

(IRAP)