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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.

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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.

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