GSK206136

GSK206136 is a small molecule drug developed by GSK (GlaxoSmithKline) as an antagonist of the neurokinin 1 receptor (NK1R). Its primary mechanism of action is to block the NK1R, which is involved in the regulation of stress and anxiety responses through its interaction with substance P, a neuropeptide. The compound was investigated for potential therapeutic use in nervous system diseases, specifically targeting anxiety disorders and depressive disorder. The first-in-human clinical trial evaluated its safety, tolerability, pharmacokinetics, and brain penetration using PET imaging in healthy male subjects[2][1][9]. As of the latest available information, development has not progressed beyond Phase 1.