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.
Response (mm)
91″ “A Iogw agonist concentration
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.
Response Response Increasingconcemfions What can you deduce about the type of antagonist used
am on E [ om on E °ftheamag°nist in each situation? [9]
Amratons Ag 81 IY J
I] the antagonist
log1D [agonist] in organ bath (M) Iogm [agonist] in organ bath (M)
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. N 0 need to plot all d-r
curves, just read the relevant data from the screen-plots [9]. Construct an Schild plot and determine the pAz. Show all
calculations.
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