Panadiplon

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Panadiplon is a nonbenzodiazepine anxiolytic drug that was developed in the 1980s. It belongs to the class of pyrazolopyrimidines and was investigated for its potential use in the treatment of anxiety disorders and insomnia.

Pharmacology

Panadiplon acts as a GABAA receptor positive allosteric modulator, which enhances the effect of the neurotransmitter GABA at the GABAA receptor. This action results in increased inhibitory effects in the central nervous system, leading to its anxiolytic and sedative properties.

Development and Clinical Trials

During its development, Panadiplon showed promise in preclinical studies and early clinical trials. However, further development was halted due to concerns about its safety profile, particularly its potential to cause hepatotoxicity.

Mechanism of Action

Panadiplon binds to a specific site on the GABAA receptor, distinct from the benzodiazepine binding site. This binding increases the frequency of chloride ion channel opening events, leading to hyperpolarization of the neuron and a decrease in neuronal excitability.

Side Effects

The most common side effects observed with Panadiplon included drowsiness, dizziness, and headache. More serious adverse effects, such as liver toxicity, were a significant concern and contributed to the discontinuation of its development.

See Also

• Anxiolytic
• GABAA receptor
• Nonbenzodiazepine
• Hepatotoxicity

External Links

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