Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
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.
Caldwell
John P
JP
CV & CNS Department of Chemical Research, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. john.caldwell@spcorp.com
Matasi
Julius J
JJ
Zhang
Hongtao
H
Fawzi
Ahmad
A
Tulshian
Deen B
DB
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
D016244:Guanosine 5'-O-(3-Thiotriphosphate); D008024:Ligands; D010880:Piperidines; D011957:Receptors, Opioid; D013141:Spiro Compounds; D000094942:Nociceptin Receptor; C000722285:Oprl1 protein, rat