Which drug has inverse agonist activity at benzodiazepine receptors?
Correct Answer: Beta carboline
Description: Benzodiazepine Binding Site Ligands: The components of the GABA A receptor-chloride ion channel macromolecule that function as benzodiazepine binding sites exhibit heterogeneity. Three types of ligand-benzodiazepine receptor interactions have been repoed: Agonists: facilitate GABA actions, and this occurs at multiple BZ binding sites in the case of the benzodiazepines. Antagonists are typified: by the synthetic benzodiazepine derivative flumazenil. Inverse agonists act as negative allosteric modulators of GABA-receptor function. Their interaction with BZ sites on the GABA A receptor can produce anxiety and seizures, an action that has been demonstrated for several compounds especially the b carbolines Naltrexone: Opioid receptor antagonist. Zopiclone: In contrast to benzodiazepines, zolpidem, zaleplon, and eszopiclone bind more selectively because these drugs interact only with GABA A -receptor isoforms that contain a1 subunits.
Category:
Pharmacology
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