FG7142

FG-7142 is a synthetic beta-carboline derivative that acts as an inverse agonist at the benzodiazepine binding site of the GABA_A receptor. It is used primarily as a research tool to induce anxiety-like states in both animal models and human studies, enabling investigation of anxiety mechanisms and the effects of anxiolytic drugs.

Mechanism and effects: By binding to the benzodiazepine site, FG-7142 reduces GABAergic inhibitory signaling, leading to increased neuronal excitability. The resulting behavioral and physiological effects are typically characterized by heightened anxiety, increased arousal, and vigilance, with potential cognitive disruption under some conditions. At higher exposures, proconvulsant or other adverse CNS effects can occur.

Research use: FG-7142 has been employed to model anxiety and to evaluate the efficacy of candidate anxiolytics, including benzodiazepine receptor ligands and other agents that modulate GABAergic transmission. It has also contributed to understanding the role of GABA_A receptor subtypes in anxiety, stress responses, and cognitive processes.

Safety and status: FG-7142 is a pharmacological research chemical and is not approved for medical use in humans. Because it can provoke significant anxiety, autonomic arousal, and potential seizures, its administration is limited to controlled laboratory settings with appropriate oversight and ethical approval. Its use is largely confined to preclinical and translational research contexts to study the benzodiazepine receptor and related anxiolytic mechanisms.