Don’t forget to refer to all sources you may have consulted (a bibliography is sufficient).
Please state your partner’s name and attach a signed statement of authorship.
Both prac-assignments together count for 25% towards subject assessment.
Questions
1. How often is length measured during an experimental cycle? [13] Why that often?
2. How does ‘occupancy’ translate into ‘response’?
3. Consider the dose-occupancy (left) and dose-response (right) curves.
Sketch how they would change with affinity and efficacy.
4. How would you, quickly, screen for differences in efficacy? Do it for all 12 agonists! Report the results and the
order of apparent efficacy.
5. What is the effect of a small amount of irreversible, competitive antagonist, when plenty of ‘spare receptors’ are
available? [15]. What then, if you keep adding antagonist?
6. Explain why the X-intercept in an Schild plot is significant. What is the slope of an Schild plot? So,
theoretically,
how many data points would you need to construct an Schild plot? [13]
7. Consider the graphs.
What can you deduce about the type of antagonist used
in each situation? [9]
8. Determine the pA2
for mepyramine. [6]. First, pick the most appropriate agonist. Use at least 3 doses
(concentrations) of antagonist and try to limit yourself to 8 doses of agonist each. Table all data. No need to plot
all d-r
curves, just read the relevant data from the screen-plots [9]. Construct an Schild plot and determine the pA
2
. Show all
calculations.
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