Drug Receptors

Question 1

Super Family: Ligand Gated Channels
Activated by:
Response time:
Found in:

Answer 1

Ligand
Milliseconds
Neurons

Question 2

Superfamily: GPCRs
Activated by: 
Response times: 
Found in:
Additional uses:

Answer 2

Exocrine ligands binding to the outside of cell membrane
Seconds
Every cell
Hormonal uses

Question 3

Superfamily: Kinase-Linked
Activated by:
Response time:
Found in:
Additional uses:

Answer 3

Cytokine or growth factor
Hours
differentiating cells
Complex cell functions

Question 4

Nuclear Receptors
Activated by:
Response time:
Found in:

Answer 4

small lipid molecules (Hormones)
hours
cytosol

Question 5

Nicotinic Acetylcholine Receptor (nAChR) is an example of what type of receptor

Answer 5

Ligand gated ion channel

Question 6

B Adrenergic receptor is an example of what type of receptor

Answer 6

G protein coupled receptor

Question 7

Epidermal Growth factor is an example of what receptor

Answer 7

Kinase linked receptor

Question 8

Mineral cortoid receptors an example of what type of receptor

Answer 8

Nuclear receptor

Question 9

Drug Binding: Define Lock and Key Design

Answer 9

Lock and key is defined by the receptor requiring an exact fit of a ligand in order for activation to occur

Question 10

Drug Binding: Law of Mass action High and low infers what about the affinity

Answer 10

High: Low affinity
Low: High affinity
Due to kd = Reverse / Forward (rates)

Question 11

Define Affinity

Answer 11

Affinity is the tendency to bind to a certain receptor

Question 12

Define Efficacy

Answer 12

Efficacy is the tendency to activate bound receptors

Question 13

Define Antagonist

Answer 13

A molecule that has affinity but no efficacy

Question 14

Define Agonist

Answer 14

A molecule that has affinity and efficacy

Question 15

EC50 means?

Answer 15

Amount of drug required to reach half maximal effect

Question 16

Emax means

Answer 16

Amount of drug required to reach maximal effect

Question 17

Potency means?

Answer 17

Measure of a drugs activity, eg more potent means less concentration required

Question 18

What is a partial agonist

Answer 18

An agonist that has a lower maximal effect than what can be achieved
Lower efficacy

Question 19

What is a full agonist

Answer 19

An agonist that can exert the maximal biological effect

Question 20

What is a competitive antagonist

Answer 20

An agonist that binds to the same orthosteric site as the agonist

Question 21

Non-competitive antagonism

Answer 21

An agonist that binds to a different binding site

Question 22

Insurmountable antagonism

Answer 22

Is irreversible changing of the target receptor

Question 23

Physiological antagonism

Answer 23

Physiological effects that functionally counter one another despite using different effector pathways
Eg. M2 Receptor stimulation Decreasing heart rate
B1 Receptor

Question 24

Selectivity means?

Answer 24

Preferential interaction with a receptor over an other

Question 25

Specificity means?

Answer 25

Specific biological effect is produced

Question 26

What is a biopharmaceutical

Answer 26

Is a drug that is produced biologically

Question 27

Advantages of biopharmaceuticals

Answer 27

Larger and more complex Made by the body Higher selectivity Chemically engineerable into other more effective drugs

Question 28

Limitations of biopharmaceuticals

Answer 28

Short half lives Administration is injected only Expensive to produce due to complexity