Inverse agonist of benzodiazepine receptor is :
Benzodiazepine receptors are part of the GABA-A receptor complex. Benzodiazepines are positive allosteric modulators, meaning they enhance the effect of GABA by increasing the frequency of chloride channel opening. So, an inverse agonist here would reduce GABA's effect, leading to excitatory effects.
Now, what are the known inverse agonists? Beta-carotene? No, that's a vitamin. Flumazenil is a competitive antagonist, used to reverse benzodiazepine overdose. It's not an inverse agonist. Then there's beta-carboline derivatives like FG-7142 or PK 11195. Wait, PK 11195 is a GABA antagonist. FG-7142 is a beta-carboline derivative that acts as an inverse agonist on benzodiazepine receptors. So FG-7142 would be the answer here.
Looking at the options, the correct answer is C. FG-7142. The other options are either antagonists or unrelated. Flumazenil is an antagonist, beta-carotene is unrelated. So the explanation should highlight the mechanism of inverse agonism versus antagonism, and the specific compounds involved.
**Core Concept**
Inverse agonists reduce the intrinsic activity of a receptor below baseline. Benzodiazepine receptors (BZD-Rs) are part of the GABA-A receptor complex; inverse agonists here decrease GABA-mediated chloride influx, causing neuronal excitation. This contrasts with **agonists** (enhance GABA) and **antagonists** (block both agonists and inverse agonists).
**Why the Correct Answer is Right**
FG-7142 is a β-carboline derivative that acts as an inverse agonist at BZD-Rs. It binds to the same site as benzodiazepines but induces conformational changes that reduce GABA’s efficacy. This leads to decreased chloride channel opening, depolarization, and increased seizure susceptibility. Its mechanism is distinct from antagonists like flumazenil, which competitively inhibit all BZD-R ligands without altering receptor activity.
**Why Each Wrong Option is Incorrect**
**Option A:** Flumazenil is a competitive antagonist, not an inverse agonist. It blocks both agonists and inverse agonists but does not activate or inhibit the receptor intrinsically.
**Option B:** Beta-carotene is a vitamin A precursor with no known activity at BZD-Rs.
**Option D:** Baclofen is a GABA-B agonist, unrelated to BZD-R function.
**Clinical Pearl / High-Yield Fact**
Inverse agonists like FG-7142 are used in research to study BZD-R function. Clinically, β-carbolines (e.g., FG-7142) may exacerbate anxiety or seizures, unlike benzodiazepines. Remember: **ant