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Pagoclone is an investigational anxiolytic drug from the cyclopyrrolone family, structurally related to zopiclone but classified as a nonbenzodiazepine. It acts as a subtype-selective modulator of the GABAA receptor, binding with high affinity to benzodiazepine sites on receptors containing α1, α2, α3 or α5 subunits. Pagoclone is a partial agonist at GABAA receptors containing α1-, α2-, and α5-subunits and a full agonist at those with an α3-subunit. This selectivity is thought to confer anxiolytic effects with minimal sedative or amnestic side effects compared to traditional benzodiazepines. The drug was developed for potential use in anxiety disorders and other indications such as stuttering and premature ejaculation but was never commercialized[2][3][4][5][6][7].
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