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

ABSTRACT: 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.

SUBMITTER: Zaveri NT

PROVIDER: S-EPMC3852901 | biostudies-literature | 2004 Jun

REPOSITORIES: biostudies-literature

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

Zaveri Nurulain T NT Jiang Faming F Olsen Cris M CM Deschamps Jeffrey R JR Parrish Damon D Polgar Willma W Toll Lawrence L

Journal of medicinal chemistry 20040601 12

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. ...[more]

PMID: 15163178

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