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Adipiplon

Adipiplon (developmental code name NG2-73) is an anxiolytic drug developed by Neurogen Corporation. It has similar effects to benzodiazepine drugs, but is structurally distinct and classed as a nonbenzodiazepine anxiolytic.

Adipiplon is a subtype-selective GABA<sub>A</sub> receptor partial agonist, which binds preferentially to the α<sub>3</sub> subtype. This is significant as while several previous nonbenzodiazepine drugs have been developed that are selective for α<sub>2/3</sub> over the other subtypes, adipiplon is one of the first drugs selected for clinical development which can discriminate between α<sub>2</sub> and α<sub>3</sub>, as well as showing a little affinity for the α<sub>1</sub> or α<sub>5</sub> subtypes — alpidem is selective for α<sub>3</sub> over α<sub>2</sub>, but still has moderate affinity for α<sub>1</sub>, whereas adipiplon is highly α<sub>3</sub>-selective with little affinity for either α<sub>1</sub>, α<sub>2</sub> or α<sub>5</sub>.

Adipiplon was being researched as a potential medication for the treatment of anxiety and insomnia, and in 2008 it was being used in Phase IIb trials. These trials were suspended after significant next-day side effects were discovered.

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