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Chapter 3: Problem 10

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.

Short Answer

Expert verified
The process would involve identifying a potential lead compound that can block the tyramine receptor, then modifying this compound to improve its effectiveness and safety. This is followed by thorough testing, with further modifications made based on the results of these tests.

Step by step solution

01

Understanding the Problem

The problem here involves creating a new antihypertensive agent (a drug used to lower blood pressure) that acts on the tyramine receptor. This receptor triggers the release of norepinephrine, which raises blood pressure. An effective antihypertensive acting on this receptor would need to inhibit this mechanism.
02

Lead Discovery

In pharmaceuticals, a 'lead' is a chemical which has effects on the body and could be developed into a drug. In this instance, we would look for leads which bind to the tyramine receptor. By studying the receptor and its interactions, we can identify potential leads. Dedicated laboratory techniques such as high-throughput screening can expedite this process. In our case, suitable leads would be compounds that have the potential to block the tyramine receptor, preventing the release of norepinephrine and therefore not elevating the blood pressure.
03

Lead Modification

Once a promising lead has been identified, it may not be perfect and could require modifications to improve its efficacy and limit its side-effects. This process, known as lead modification or lead optimization, could involve changes to the chemical structure of the lead to improve its binding to the tyramine receptor, increasing its efficacy at lower doses, or making it more stable and easier to administer.
04

Testing and Further Modification

Any potential drug must go through thorough testing for safety and efficacy. Initially, this might involve laboratory tests and animal trials. The information from these tests can be used to make further modifications to the lead compound. If the results are promising, the compound will proceed to clinical trials in humans.

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