A novel series of piperidin-4-yl-1, 3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor

NT Zaveri, F Jiang, CM Olsen… - Journal of medicinal …, 2004 - ACS Publications
NT Zaveri, F Jiang, CM Olsen, JR Deschamps, D Parrish, W Polgar, L Toll
Journal of medicinal chemistry, 2004ACS Publications
A series of N-(4-piperidinyl)-2-indolinones were discovered as a new structural class of
nociceptin receptor (NOP) ligands. Unlike other previously reported classes of NOP receptor
ligands, modifications of the piperidine N substituents afforded both potent agonists and
antagonists, with modest selectivities over other opioid receptors. The SAR revealed in this
new series will provide important insights for the development of pharmacophores for
agonist and antagonist actions at the NOP receptor.
A series of N-(4-piperidinyl)-2-indolinones were discovered as a new structural class of nociceptin receptor (NOP) ligands. Unlike other previously reported classes of NOP receptor ligands, modifications of the piperidine N substituents afforded both potent agonists and antagonists, with modest selectivities over other opioid receptors. The SAR revealed in this new series will provide important insights for the development of pharmacophores for agonist and antagonist actions at the NOP receptor.
ACS Publications