title: 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.
authors.affiliation: Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA. nurulain.zaveri@sri.com
authors.forename: Nurulain T
authors.initials: NT
authors.lastname: Zaveri
authors.forename: Faming
authors.initials: F
authors.lastname: Jiang
authors.forename: Cris M
authors.initials: CM
authors.lastname: Olsen
authors.forename: Jeffrey R
authors.initials: JR
authors.lastname: Deschamps
authors.forename: Damon
authors.initials: D
authors.lastname: Parrish
authors.forename: Willma
authors.initials: W
authors.lastname: Polgar
authors.forename: Lawrence
authors.initials: L
authors.lastname: Toll
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D009292:Narcotic Antagonists; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D011957:Receptors, Opioid / Q000819:agonists*; D013329:Structure-Activity Relationship; D000094942:Nociceptin Receptor
chemical_list: D007211:Indoles; D008024:Ligands; D009292:Narcotic Antagonists; D010880:Piperidines; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor