Lecture 32 & 33

Question 1

Weak agonists will inject a small signal transduction.

Does the compound with the highest affinity necessarily be the drug that, at given concentration, will give the greatest response?

Answer 1

No, the highest response can be from one with less affinity, as the compound also has to be able to induce a signal transduction from the receptor - measured as intrinsic efficacy3

Question 2

A full agonist…

Answer 2

causes a maximal response

Question 3

A partial agonist

Answer 3

may cause a lesser response when all the receptors are occupied

Question 4

Intrinsic efficacy is…

Answer 4

the stimulus generated upon receptor binding - property of the drug

Question 5

In a drug binds to a receptor, but does not elicit a response, it is a

Answer 5

antagonist

Question 6

What is coupling efficiency?

Answer 6

efficiency of the stimulation of the drug binding to the receptor

ie. how much the change in shape of the receptor, will lead to the signal transduction pathway.

Question 7

True or False

Concentration/response curves cannot show the affinity of a drug

Answer 7

True

Question 8

True or False:

Prenalterol will give a greater response in the gut than in the atria

Answer 8

False

other way around - lesser response

Question 9

What happens in drug de-sensitisation?

Answer 9

check

Question 10

For high potency, we need high:

________
________

Answer 10

affinity and efficacy

Question 11

Antagonism involves

Answer 11

directly binding, or destroying the other molecule

Question 12

True or False.

Only one drug molecule can bind to the active site of a receptor at a time

One drug bound prevents another from binding

Answer 12

True