Adipiplon

Adipiplon.svg

Adipiplon is a nonbenzodiazepine hypnotic and anxiolytic drug that was under development for the treatment of insomnia and anxiety disorders. It acts as a GABAA receptor agonist, specifically targeting the α3 subunit of the receptor, which is believed to be associated with the drug's anxiolytic effects.

Mechanism of Action

Adipiplon works by enhancing the activity of the gamma-aminobutyric acid (GABA) neurotransmitter at the GABAA receptor. This receptor is a ligand-gated ion channel that, when activated, allows the influx of chloride ions into the neuron, leading to hyperpolarization and decreased neuronal excitability. By selectively targeting the α3 subunit, adipiplon aims to provide anxiolytic effects with potentially fewer side effects compared to non-selective GABAA receptor agonists.

Clinical Development

Adipiplon was being developed by Neurogen Corporation for the treatment of insomnia and anxiety disorders. However, its development was discontinued after clinical trials. The reasons for discontinuation included issues related to efficacy, safety, and tolerability.

Pharmacokinetics

The pharmacokinetic profile of adipiplon includes its absorption, distribution, metabolism, and excretion. Adipiplon is administered orally and undergoes hepatic metabolism. The primary route of excretion is through the renal system.

Side Effects

Common side effects of adipiplon observed in clinical trials included drowsiness, dizziness, and headache. As with other GABAA receptor agonists, there is a potential for dependence and withdrawal symptoms upon discontinuation.

See Also

• Nonbenzodiazepine
• GABAA receptor
• Insomnia
• Anxiety disorder
• Neurogen Corporation

External Links

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