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Which of the following theoretical drugs would BEST classify as a partial agonist?
a) A drug that binds 2 separate receptors causing an effect at one and no effect at the other
b) A drug that binds one receptor and triggers the innate activity of that receptor, but the innate response does not clinically affect the patient
c) A drug that blocks all transmission from the synaptic junction
d) A drug that causes a mild decrease in pain perception
e) A drug that binds a receptor and triggers a sub-maximal response of the same type as the innate activity.
Answer
Answer e. Unlike antagonists, which bind and cause no effect at the receptor (but prevent other substances from binding), a partial agonist does have some agonism that mimicks the innate effect, but to a lesser extent. These drugs may also be thought of as partial antagonists, in that they do prevent the binding of a potent agonist and thereby reduce the maximal possible effect to some extent.
Notes
- This question originally printed in the Pediatric Anesthesiology Review Topics kindle book series, and appears courtesy of Naerthwyn Press, LLC.