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NBME 24 Answers

nbme24/Block 3/Question#29 (reveal difficulty score)
Drug X is given to a 25-year-old normal ...
Partial agonist at ฮฒ-adrenergic receptors ๐Ÿ” / ๐Ÿ“บ / ๐ŸŒณ / ๐Ÿ“–
tags: pharm repeat

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 +17  upvote downvote
submitted by โˆ—tea-cats-biscuits(273)

Partial agonists have weak agonist activity on their own (thus in this case it causes HR to increase, b-adrenergic effect) but when an actual agonist is present (aka when you are exercising, you are producing NE and E that have full b-agonist effects), partial agonist actually have a mild antagonist effect (thus the heart rate decreases).

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potentialdoctor1  Might be relevant to add that there are two beta-blockers that are actually partial beta-agonists (exert their blocking effects due to lesser effect when compared with endogenous catecholamines) ----> Pindolol and acebutolol +10
thelupuswolf  Key to note as madojo said that a partial agonist will compete with the full agonist in the presence of the full agonist, preventing the full agonist's maximum effect +

 +6  upvote downvote
submitted by โˆ—madojo(212)

A key property of partial agonists is that they display both agonistic and antagonistic effects. In the presence of a full agonist , a partial agonist will act as an antagonist, competing with the full agonist for the same receptor and thereby reducing the ability of the full agonist to produce its maximum effect. Ex. Morphine (full agonist) vs buprenorphine (partial agonist) at opioid mu receptors 234 FA 19

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 +0  upvote downvote
submitted by theunscrambler(4)

Partial agonist:,to%20produce%20its%20maximum%20effect.

In the case of exercise, there is increased sympathetic tone (acts as full agonist).

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