title: Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.
abstract: A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure-activity relationships have been explored around the 3-phenoxypropyl region with several potent and selective analogues identified.
authors.affiliation: Department of Medicinal Chemistry, Organon Laboratories Ltd, Newhouse, Lanarkshire ML1 5SH, UK. r.palin@organon.co.uk
authors.forename: Ronald
authors.initials: R
authors.lastname: Palin
authors.forename: David R
authors.initials: DR
authors.lastname: Barn
authors.forename: John K
authors.initials: JK
authors.lastname: Clark
authors.forename: Jean E
authors.initials: JE
authors.lastname: Cottney
authors.forename: Phillip M
authors.initials: PM
authors.lastname: Cowley
authors.forename: Marc
authors.initials: M
authors.lastname: Crockatt
authors.forename: Louise
authors.initials: L
authors.lastname: Evans
authors.forename: Helen
authors.initials: H
authors.lastname: Feilden
authors.forename: Richard R
authors.initials: RR
authors.lastname: Goodwin
authors.forename: Frank
authors.initials: F
authors.lastname: Griekspoor
authors.forename: Simon J A
authors.initials: SJ
authors.lastname: Grove
authors.forename: Andrea K
authors.initials: AK
authors.lastname: Houghton
authors.forename: Philip S
authors.initials: PS
authors.lastname: Jones
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Morphy
authors.forename: Alasdair R C
authors.initials: AR
authors.lastname: Smith
authors.forename: Hardy
authors.initials: H
authors.lastname: Sundaram
authors.forename: David
authors.initials: D
authors.lastname: Vrolijk
authors.forename: Mark A
authors.initials: MA
authors.lastname: Weston
authors.forename: Grant
authors.initials: G
authors.lastname: Wishart
authors.forename: Paul
authors.initials: P
authors.lastname: Wren
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D000242:Cyclic AMP / Q000096:biosynthesis; D015195:Drug Design; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D008297:Male; D051379:Mice; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000819:agonists*; D013329:Structure-Activity Relationship; D014162:Transfection; D014649:Vas Deferens; D000094942:Nociceptin Receptor
chemical_list: D010880:Piperidines; D011957:Receptors, Opioid; D000242:Cyclic AMP; D000094942:Nociceptin Receptor