1- What are the two key properties of receptor function.
2- Why is a drug with a lower Kd more potent than one with a higher Kd?
3- Why is intramolecular hydrogen bonding so important in drug design?
4- Compound 4 is a much more potent antagonist for the a1-adrenergic receptor than 5. Compound 6 is almost as potent as 4. Give two rationalizations for this observation.
5- What is a competitive antagonist?
6- Why can two enantiomers of the same molecule have different binding affinities for the same receptor binding site?
7- If the eudismic ratio is low, what two conclusions can you make? (not in pharmacophore; not specific drug)
8- Why does administration of racemates generally lead to more side effects than the eutomer?
9- What are conformationally-rigid analogues and what are they used for?
10- Compounds A and B agonize the PPAR receptor. Dose response curves of the two compounds were constructed, and it was found that the Kd for A 20 nM and for B was 90 nM. As best you are able, draw dose-response curve (on the same plot) for these two compounds (label the axes).