The following question relates to the following pA₂ values for a series of antagonists at serotonin (5-HT) receptor subtypes.

According to the listed pA2 values, which one of the following concentrations of Compound 02 could be used to block 5-HT3 receptors, without also blocking 5-HT1d?

The following questions relate to the following pA₂ values for a series of antagonists at serotonin (5-HT) receptor subtypes.

Which one of the following BEST represents the potency profile of Compound 02 at each receptor subtype?

Which one of the listed compounds shows the HIGHEST potency at 5-HT1d receptors?

5-HT3 receptor antagonists can be used to treat nausea, but can cause unwanted effects at 5-HT2 receptors on platelets.  If you wanted to develop a new 5-HT3 antagonist that is unlikely to interact with 5-HT2 receptors, which one of the listed compounds would be the BEST choice?

George, a 42 year-old man has been diagnosed with hypercholesterolemia. His physician prescribes the statin, atorvastatin.  After several weeks, George returns to his physician complaining of muscle pain, tenderness and weakness.  His physician also notices that George has yellowing eyes and skin.  George’s plasma cholesterol levels had however, returned to within the normal range. 

Which one of the following MOST LIKELY accounts for George’s symptoms?

George’s physician made enquiries regarding his diet and found that he consumed grapefruit juice on a daily basis.  He was instructed to continue taking atorvastatin but to stop drinking grapefruit juice.  George’s symptoms disappeared but his plasma cholesterol levels remained well controlled. 

Using the Flockhart chart, explain the interaction between grapefruit juice and atorvastatin.

CYP450:

A radioligand binding experiment was carried out to screen several new compounds at 5-HT receptor subtypes.

Based on these IC50 values, which one of the following can you conclude about Compound EAD04?  Compound EAD04 has the highest:

Based on these IC50 values, which one of these new compounds is MOST selective for the 5-HT2a receptor subtype?

Drug A is an active anti-epileptic drug with pharmacokinetic parameters shown in the table below. 

Pharmacokinetic analysis of Drug A taken in combination with a herbal supplement (extract A) was performed and tabulated as shown above.

Extract A is MOST LIKELY altering the pharmacokinetics of Drug A by which one of the following mechanisms?

What is the MOST LIKELY clinical consequence of taking Drug A with this herbal extract?