83093 BI2BE4

a).

The maximal responses (in %) from Table 1 were calculated for each log agonist concentration. Using
(𝑚𝑚) 𝑟𝑒𝑠𝑝𝑜𝑛𝑠𝑒 𝑎𝑓𝑡𝑒𝑟 𝑒𝑎𝑐ℎ log 𝑐𝑜𝑛𝑐𝑒𝑛𝑡𝑟𝑎𝑡𝑖𝑜𝑛
the formula: × 100
20 mm (maximum response)

Table 1: The smooth muscle contraction (%) after adding each agonist and their concentrations (M)
Table 1 This table shows the smooth muscle response regarding contraction (in %) for each of the agonists and their concentrations. The higher the
concentration of the agonists, the higher the response. Agonist 2 is a partial agonist, whilst Agonists 1 and 3 are full agonists.

Figure 1 This graph shows the contractile response (%) caused by increasing concentrations of the agonist. Agonists 1 and 3
had a higher efficacy than Agonist 2, whilst Agonist 1 was the most potent and Agonist 3 was the least potent of the 3
agonists. The EC50 values were calculated from seeing the 50% response from the y axis and drawing a line and then
drawing a line towards the x axis.

Agonists 1 and 3 are both full agonists because they achieve the maximal contractile response (%).
Whilst Agonist 2 is a partial agonist because it does not achieve the maximal contractile response.
Agonists 1 and 3 have an equal Emax (they achieve the same maximum response of 100%), whilst
Agonist 2 achieves a lower Emax and a maximum response of 50%. Due to this, Agonists 1 and 3
have a higher Efficacy, whilst Agonist 2 has a lower efficacy. Agonist 1 requires the lowest log
 83093 BI2BE4

concentration of agonist (1 × 10−8 𝑀) to achieve half the maximal response meaning it has the
lowest EC50. Agonist 2 requires the second lowest log concentration (1 × 10−7 𝑀) to achieve half
the maximal response and therefore has the second lowest EC50 Agonist 3 requires the highest log
concentration (1 × 10−6 𝑀) to achieve half the maximal response and therefore has the lowest
EC50. This means that Agonist 1 is the most potent, followed by Agonist 2 and Agonist 3 is the least
potent.

b).

i).

Table 2: Smooth muscle response by an agonist in the presence of an Antagonist:

Table 2 displays the smooth muscle response (mm) after adding increasing log concentrations (M) in the presence of an Antagonist
𝑅𝑒𝑠𝑝𝑜𝑛𝑠𝑒 (𝑖𝑛 𝑚𝑚)
concentrations in (M). These values were calculated by × 100.
30 𝑚𝑚

Figure 2 is a graph that shows the smooth muscle response

(%) after adding log (agonist concentration) (M) in the
presence of Antagonist concentrations (M)
83093 BI2BE4

ii)

Table 3 showing the log Antagonist concentration (M) and EC50 values in M taken from Figure 2. The dose ratio and Log
(Dose Ratio-1) was calculated using these EC50 values. Calculations are shown in figure 3 and 4.

Figure 3 The top image shows how the

iii). EC50 value in M is calculated for the
Agonist without the presence of an
Antagonist. The bottom image shows
how the EC50 value in M is calculated for
the Agonist in the presence of an
Antagonist.
83093 BI2BE4

Figure 4 shows on the left of the

image how the Dose ratio is
calculated and on the right of the
image shows how Log (Dose Ratio-1)
is calculated.

(iii).

iii).

Figure 5 shows a Schild plot graph to work out the Kb value. The X axis shows the Log Antagonist concentration in M, and
the Y axis shows the Log (Dose Ratio-1) values. The Kb is the Log(antagonist concentration) in M where the line crosses the X
axis.
83093 BI2BE4

Kb is the dissociation equilibrium constant of the receptor and antagonist complex. The Kb
value correlates to the concentration of antagonist when half of the receptors have an
antagonist molecule bound to them. It is also the concentration of antagonist giving a dose
ratio of 2 (meaning the agonist concentration needs to be twice as much to give the same
effect). The gradient of the line from the Schild plot is approximately 1 and the line is
straight, therefore the antagonist is reversible and competitive.