Question:medium
Which of the following is an inverse agonist at the benzodiazepine receptor?
Which of the following is an inverse agonist at the benzodiazepine receptor?
Show Hint
Look for the anxiogenic and proconvulsant agent that does the opposite of diazepam.
Updated On: Jun 24, 2026
- Phenobarbitone
- Flumazenil
- Beta carboline
- Gabapentin
Show Solution
The Correct Option is C
Solution and Explanation
Step 1: Picture the BZD recognition pocket on the GABA-A receptor as a switch that can be pushed in three directions. Push it one way (full agonist) and inhibitory chloride flow rises, giving calm and sleep. Leave it neutral (antagonist) and nothing changes on its own. Push it the other way (inverse agonist) and chloride flow falls below baseline, which translates clinically into restlessness, anxiety and seizures.
Step 2: Among the listed drugs, the beta carbolines occupy exactly that opposite, negative-efficacy end of the spectrum. By lowering GABA-driven inhibition they are anxiogenic and convulsant, the textbook signature of an inverse agonist.
Step 3: Checking the rest: flumazenil only sits in the pocket and blocks it (antagonist used to reverse BZD overdose), phenobarbitone works through the barbiturate site, and gabapentin works on a calcium channel subunit. None of them flips the receptor in the negative direction.
\[\boxed{\text{Beta carboline}}\]
Step 2: Among the listed drugs, the beta carbolines occupy exactly that opposite, negative-efficacy end of the spectrum. By lowering GABA-driven inhibition they are anxiogenic and convulsant, the textbook signature of an inverse agonist.
Step 3: Checking the rest: flumazenil only sits in the pocket and blocks it (antagonist used to reverse BZD overdose), phenobarbitone works through the barbiturate site, and gabapentin works on a calcium channel subunit. None of them flips the receptor in the negative direction.
\[\boxed{\text{Beta carboline}}\]
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