NS11821

NS11821 is a small molecule, partial subtype-selective GABAA receptor agonist and positive allosteric modulator developed by NeuroSearch for the treatment of anxiety disorders. It was designed to selectively target the alpha-2, alpha-3, and alpha-5 subunits of the GABAA receptor while maintaining negligible activity at the alpha-1 subunit. This pharmacological profile was intended to provide anxiolytic and potentially cognitive-enhancing effects without the sedation, ataxia, and dependence associated with non-selective benzodiazepines. NS11821 reached Phase I clinical development, where it was evaluated in a first-in-human, single ascending oral dose study in healthy volunteers. However, the development of the compound was subsequently terminated.