You perform a competition study on a GPCR. You have isolated the plasma membrane from cells which contains the GPCR of interest. If an agonist and an inverse agonist are at equal concentrations in your study but the inverse agonist has a 10 x higher affinity for the receptor than the agonist, what would you expect to be the overall outcome to be? More of the agonist is bound and so most of the receptor is in its active conformation and is stimulated More of the inverse agonist is bound and so most of the receptor is in its inactive conformation and is unstimulated.

Human Anatomy & Physiology (11th Edition)
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Author:Elaine N. Marieb, Katja N. Hoehn
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Chapter1: The Human Body: An Orientation
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You perform a competition study on a GPCR. You have isolated the plasma membrane
from cells which contains the GPCR of interest. If an agonist and an inverse agonist
are at equal concentrations in your study but the inverse agonist has a 10 x higher
affinity for the receptor than the agonist, what would you expect to be the overall
outcome to be?
More of the agonist is bound and so most of the receptor is in its active conformation and is
stimulated
More of the inverse agonist is bound and so most of the receptor is in its inactive
conformation and is unstimulated.
Transcribed Image Text:You perform a competition study on a GPCR. You have isolated the plasma membrane from cells which contains the GPCR of interest. If an agonist and an inverse agonist are at equal concentrations in your study but the inverse agonist has a 10 x higher affinity for the receptor than the agonist, what would you expect to be the overall outcome to be? More of the agonist is bound and so most of the receptor is in its active conformation and is stimulated More of the inverse agonist is bound and so most of the receptor is in its inactive conformation and is unstimulated.
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