Professional Documents
Culture Documents
Workshop Cellular Pharmacology: Pharmacology
Workshop Cellular Pharmacology: Pharmacology
Workshop Cellular Pharmacology: Pharmacology
concentration of binding
ligand (nM) (cpm)
10.00 280
7.00 301
3.00 240
1.80 205
1.50 171
1.20 127
0.60 70
0.00 0
2. Two drugs have been tested for their properties to cause a cellular response.
See the data below.
a) Using graph paper, plot a log concentration response curves for drug A and B
b) Estimate the EC50 values for both drugs
c) Which drug is more potent and which is more efficacious? Explain your answer
3. This is the result for a saturation binding experiment. Plot a saturation curve.
Estimate Kd and Bmax for the ligand.
concentration of binding
ligand (nM) (cpm)
10.00 100.
7.00 98.
5.00 95.
3.00 85.
1.80 70.
1.50 60.
1.20 48.
0.60 30.
0 0
4. Two drugs have been tested for their properties to cause a cellular response.
See the data below. Which one is the more potent drug? Which one is more
efficacious?
a) Using graph paper, plot a log concentration response curves for both drugs
b) Estimate the EC50 values for the drugs
5. Dose response data was collected during the preclinical testing of four drugs for
the treatment of acute heart failure. Which drug studied was the most efficacious?
8. Drugs with low efficacy bind to receptors but do not fully activate them. Such
"partial agonists" can act as either as a weak agonist (in the absence of a full
agonist), or as a competitive antagonist (if a full agonist is present). Which curve best
reflects the effect produced by this type of agonist when it is administered alone?
9. Plot representative concentration-response curves for EACH of the following:
150
A
100 B
50 C
0 D
-50
-100
-150
-200
-10 -9 -8 -7 -6 -5
ligand concentration log [M]
11. This graph illustrates the dose-response relationship for the effect of the beta
agonist isoproterenol on an isolated perfused heart, both alone and in the presence
of different fixed concentrations of Drug X. Based upon the data shown, Drug X is
most likely a(n):
13) Give a definition for the pA2 value and the dose ratio
14) In an experiment, an antagonist is added to drug A above at a concentration of
200nM. The dose ratio observed in this experiment is 2. What is the pA2 value of the
antagonist?
15) In further experiments, different antagonists are used which show different pA2
values.
Which of these is the most potent antagonist? Briefly explain your answer?
16) Below is a table with different examples of Kd, which drug has the highest
affinity for the receptor? Explain your answer
Drug Kd (nM)
A 3
B 2.5
C 30
D 45
E 60