1396788-43-4Relevant articles and documents
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists
Jiang, Rong,Song, Xinyi,Bali, Purva,Smith, Anthony,Bayona, Claudia Ruiz,Lin, Li,Cameron, Michael D.,McDonald, Patricia H.,Kenny, Paul J.,Kamenecka, Theodore M.
, p. 3890 - 3894 (2012/07/13)
A series of orexin receptor antagonists was synthesized based on a substituted piperidine scaffold. Through traditional medicinal chemistry structure-activity relationships (SAR), installation of various groups at the 3-6-positions of the piperidine led to modest enhancement in receptor selectivity. Compounds were profiled in vivo for plasma and brain levels in order to identify candidates suitable for efficacy in a model of drug addiction.