Chapter 3: Problem 3
Draw a dose-response curve for: a. a full agonist b. a mixture of a full agonist and a competitive antagonist
Chapter 3: Problem 3
Draw a dose-response curve for: a. a full agonist b. a mixture of a full agonist and a competitive antagonist
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Get started for freeAn isosteric series of compounds shown below, where \(\mathrm{X}=\mathrm{CH}_{2}, \mathrm{NH}, \mathrm{O}, \mathrm{S}\), was synthesized. The order of potency was \(\mathrm{X}=\mathrm{NH}>\mathrm{O}>\mathrm{S}>\mathrm{CH}_{2}\). How can you rationalize these results (you need to consider the threedimensional structure)?
a. What problems are associated with administration of racemates? b. How can you increase the eudismic ratio?
Design conformationally-rigid analogs for: a. 4 -aminobutyric acid (GABA) b. Epinephrine c. Nicotine
Draw dose-response curves (place on same plot) for a series of three compounds with the following properties: $$ \begin{array}{lll} & K_{\mathrm{d}}(M) & \alpha \\ \hline \mathbf{1} & 10^{-6} & 1.0 \\ \hline \mathbf{2} & 10^{-9} & 0.8 \\ \hline 3 & 10^{-9} & 0.4 \\ \hline \end{array} $$
Tyramine binds to a receptor that triggers the release of norepinephrine, which can raise the blood pressure. If the tyramine receptor was isolated, and you wanted to design a new antihypertensive agent, discuss what you would do in terms of lead discovery and modification.
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