Below is the molecular structure for heroin which is the agonist for a certain t

Question

Below is the molecular structure for heroin which is the agonist for a certain type of opiate receptor. If you were a drug designer, discuss a general and reasonable approach you might use to design a competitive antagonist for this receptor. Then assuming you have been successful in your drug development, discuss a properly designed experiment you would conduct to test the effectiveness of your drug. Identify your independent and dependent variables (Note that you do need to know or describe the specific chemistry of the molecule below)

Explanation / Answer

The competitive antagonist will bind to the receptor based on structural similarity to the agonist. So we must design the molecule which is based on the lock and key model, a molecule which is similar to heroin that will bind to the receptor and not allow heroin binding. Before clinical trials, binding affinity studies must be performed. As we see there is a nitrogen atom, we can use Radioactive Nitrogen labeled antagonist to study binding, we will vary the relative concentrations of heroin and our designed antagonist to determine the efficiency and efficacy of the drug.

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