...In the presence of increasing amounts of drug X Drug X is a newly developed a
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...In the presence of increasing amounts of drug X
Drug X is a newly developed antagonist proposed for use in heart disease management that you are asked to test in the isolated rat heart model known as a Langendorff preparation, in which the heart is attached to an apparatus that allows the heart to continue to function even though it's outside the body. During laboratory investigations, the following data is obtained (the blue line represents the agonist administered alone, the red lines represent the agonist in the presence of increasing amounts (designated by the numbers provided) of Drug X). 1.0 Antagonist concentration 0.5 10 102 10 1 10 102 Agonist ooncontration On the basis of this data alone, what kind of antagonist is Drug X? Explain your answer.Explanation / Answer
On the basis of the data we can say the drug X is a non-competitive antagonist.
Non-competitive antagonists don't compete with the agonists. They allosterically change the conformation of the receptor so the agonists can't bind with them. In such antagonism, the action of agonists can't be enhanced by increasing the concentration of agonists.
From the graph it is clear that higher agonist concentration can't reach it to highest occupancy level because the receptors are conformationally changed.
In case of competitive antagonism, the action of agonists can reach to the highest occupancy level by increasing its concentration.
From the above interpretation, we can say the drug X is a non-competitive antagonist.
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