title: Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
abstract: A series of N-substituted analogs based upon the spiropiperidine core of 1 was synthesized and exhibited high binding affinity to the nociceptin (NOP) receptor. The selectivities against other known opioid receptors were determined.
authors.affiliation: CV & CNS Department of Chemical Research, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. john.caldwell@spcorp.com
authors.forename: John P
authors.initials: JP
authors.lastname: Caldwell
authors.forename: Julius J
authors.initials: JJ
authors.lastname: Matasi
authors.forename: Hongtao
authors.initials: H
authors.lastname: Zhang
authors.forename: Ahmad
authors.initials: A
authors.lastname: Fawzi
authors.forename: Deen B
authors.initials: DB
authors.lastname: Tulshian
mesh_terms: D000284:Administration, Oral; D000818:Animals; D003371:Cough / Q000188:drug therapy; D004353:Drug Evaluation, Preclinical; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D008024:Ligands; D010599:Pharmacokinetics; D010880:Piperidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D011485:Protein Binding; D051381:Rats; D011957:Receptors, Opioid / Q000819:agonists* / Q000378:metabolism; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D013329:Structure-Activity Relationship; D000094942:Nociceptin Receptor
chemical_list: D016244:Guanosine 5'-O-(3-Thiotriphosphate); D008024:Ligands; D010880:Piperidines; D011957:Receptors, Opioid; D013141:Spiro Compounds; D000094942:Nociceptin Receptor; C000722285:Oprl1 protein, rat