Lecture 5 - Mechanism of Drug Action

Question 1

Four primary drug targets?

Answer 1

ion channels, enzymes, carrier molecules, receptors

Question 2

Four step process of synaptic transmission?

Answer 2

NT synthesis, NT release, action on receptors, inactivation

Question 3

Targets of synthesis?

Answer 3

choline transporer, acetyl-coline transferase

Question 4

Targets for release?

Answer 4

ion channel blockage, prevent vesicle formation

Question 5

Four families of receptors?

Answer 5

Ion channels, GPCR, cytokine receptors and nuclear receptorsq

Question 6

Three important properties of ion channels?

Answer 6

activated in response to specific ligand, allow ion passage through impermeable membranes, selective of ions

Question 7

Muscarinic receptors and relevant G proteins?

Answer 7

1, 3 & 5 - Gq; 2 & 4 - Gi

Question 8

Pre-synaptic receptors?

Answer 8

Gi linked, inhibit Ca2+ channels, feedback loop to decrease NT, blockage can 10x increase release

Question 9

E.g of GPCR drugs?

Answer 9

adenosine, dopamine, seratonin, cannabanoid

Question 10

Tyrosine kinase receptors?

Answer 10

enzyme transferring phosphate group from ATP to tyrosine - mediates growth factor, cytokines and hormones

Question 11

Drug to receptor binding forces?

Answer 11

Vander waals (weak), hydrogen bonds (strong), ionic (stronger), covalent (strongest).