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Pagoclone is an anxiolytic agent belonging to the cyclopyrrolone family, closely related to more widely recognized medications like the sleep aid zopiclone. Initially synthesized by a French research team at Rhone-Poulenc & Rorer S.A., Pagoclone is classified as a nonbenzodiazepine, which offers effects similar to those of traditional benzodiazepines but features distinct chemical structures.

This compound binds with a notably high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABAA receptors that contain either an α1, α2, α3, or α5 subunit. Pagoclone acts as a partial agonist at the α1, α2, and α5-containing GABAA receptors, while functioning as a full agonist at receptors with an α3 subunit. In studies involving rats, 5′-hydroxypagoclone emerged as a significant metabolite, exhibiting considerably greater efficacy at the α1 subtype compared to the parent compound. This metabolite has demonstrated notable anxiolytic-like activity and the ability to induce sedation.

Unlike zopiclone, pagoclone provides anxiolytic effects with minimal sedative or amnestic properties at lower doses (ranging from 0.3 mg to 1.2 mg per day). This makes it an appealing option for those seeking relief from anxiety without the heavy sedation often associated with other medications.

Pharmacologist David Nutt has proposed that Pagoclone could serve as a foundation for developing a more effective social drug, as it elicits positive effects similar to those of alcohol, including relaxation and enhanced sociability. This potential could open new avenues for therapeutic applications in social anxiety and related disorders.

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Pagoclone 10 MG Pellets stock last updated at: April 2025

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