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Antaganonist
Antaganonist
1. Competitive Antagonists:
- Maintain the receptor in its inactive state by interfering with agonist binding.
- Shift the agonist dose-response curve to the right (increased EC50) without affecting Emax.
2. Irreversible Antagonists:
3. Allosteric Antagonists:
4. Functional Antagonism:
These definitions provide a comprehensive understanding of the different types of antagonists and their
mechanisms of action.
Certainly! When we say that a competitive antagonist shifts the agonist dose-response curve to the right without
affecting Emax, it means that the antagonist reduces the potency of the agonist without altering the maximum
response that can be achieved (Emax). Let's break it down:
- The agonist dose-response curve illustrates the relationship between the concentration of an agonist and the
response it produces.
- Typically, as the agonist concentration increases, the response also increases, reaching a maximum response
(Emax) at higher concentrations.
2. Shift to the Right:
- When a competitive antagonist is present, it competes with the agonist for the same binding site on the
receptor.
- This competition reduces the availability of the receptor for the agonist.
- As a result, higher concentrations of the agonist are required to achieve the same response as in the absence
of the antagonist.
- The agonist dose-response curve is shifted to the right along the concentration axis.
3. Increased EC50:
- The EC50 (half-maximal effective concentration) is the concentration of the agonist that produces a response
halfway between the baseline and maximum response.
- The increased EC50 indicates that a higher concentration of the agonist is needed to achieve the same
response that was achieved at a lower concentration in the absence of the antagonist.
4. Emax Unaffected:
- The Emax represents the maximum response that can be elicited by the agonist.
- In the presence of a competitive antagonist, although higher agonist concentrations are needed to achieve
the same response, the maximum response remains unchanged.
- The antagonist does not affect the ability of the agonist to produce the maximum achievable response, only
the concentration needed to reach that point.
In summary, a competitive antagonist causes a rightward shift in the agonist dose-response curve by increasing
the EC50 value. This shift indicates a reduced potency of the agonist due to competition with the antagonist.
However, the maximum response (Emax) that can be achieved by the agonist remains unaffected.