S-17092

S-17092 is a potent, selective, orally active prolyl endopeptidase (PEP) inhibitor with an IC50 of 1.2-8.3 nM. It was developed by **Servier** as a potential therapeutic agent for cognitive disorders associated with cerebral aging and neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. By inhibiting PEP, S-17092 retards the degradation of neuroactive peptides including substance P (SP) and alpha-melanocyte-stimulating hormone (alpha-MSH), which are involved in cognitive functions. The compound demonstrated nootropic effects in preclinical studies, improving performance in various memory tasks including short-term, long-term, reference, and working memory in aged mice, rodents with chemically-induced amnesia, and monkeys. In clinical studies with elderly healthy volunteers, S-17092 showed dose-dependent inhibition of plasma PEP activity, increased alpha band EEG activity at 100 mg, and improved delayed verbal memory tasks at 1200 mg dose. The compound has a terminal half-life ranging from 7-31 hours and is suitable for once-daily dosing[1][2][3][4][5][7].

Other names

2S,3aS,7aS-1-[(R,R)-2-phenylcyclopropyl]carbonyl-2-[(thiazolidin-3-yl)carbonyl]octahydro-1H-indole