Question:
Which of the following is an inverse agonist at the benzodiazepine receptor?
Which of the following is an inverse agonist at the benzodiazepine receptor?
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Look for the anxiogenic and proconvulsant agent that does the opposite of diazepam.
Updated On: Jun 24, 2026
- Phenobarbitone
- Flumazenil
- Beta carboline
- Gabapentin
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The Correct Option is C
Solution and Explanation
Step 1: The GABA-A receptor complex carries a benzodiazepine (BZD) binding site that can be engaged by three functional classes of ligand. Agonists (the classical BZDs) increase the frequency of chloride channel opening and produce sedation and anxiolysis. An antagonist simply blocks the site. An inverse agonist binds the same site but produces the opposite effect, reducing chloride conductance and causing anxiety and convulsions.
Step 2: Beta carbolines are the prototype inverse agonists at the BZD receptor. They reduce GABA-A mediated inhibition, so they are anxiogenic and proconvulsant. This makes option c correct.
Step 3: Flumazenil is a pure antagonist (it reverses BZD overdose but has no intrinsic effect of its own), so it is not an inverse agonist. Phenobarbitone acts at the barbiturate site, not as a BZD inverse agonist. Gabapentin is a gabapentinoid that modulates the alpha-2-delta calcium channel subunit and has no inverse agonist action at the BZD site.
Step 2: Beta carbolines are the prototype inverse agonists at the BZD receptor. They reduce GABA-A mediated inhibition, so they are anxiogenic and proconvulsant. This makes option c correct.
Step 3: Flumazenil is a pure antagonist (it reverses BZD overdose but has no intrinsic effect of its own), so it is not an inverse agonist. Phenobarbitone acts at the barbiturate site, not as a BZD inverse agonist. Gabapentin is a gabapentinoid that modulates the alpha-2-delta calcium channel subunit and has no inverse agonist action at the BZD site.
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