Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists

A series of potent and soluble ORL1 agonists was prepared and evaluated. Compound 41 showed antinociceptive properties in mouse formalin paw test (ED 50 = 1.07 μmol/kg). A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure–activity relation...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 15; no. 3; pp. 589 - 593
Main Authors:	Palin, Ronald, Barn, David R., Clark, John K., Cottney, Jean E., Cowley, Phillip M., Crockatt, Marc, Evans, Louise, Feilden, Helen, Goodwin, Richard R., Griekspoor, Frank, Grove, Simon J.A., Houghton, Andrea K., Jones, Philip S., Morphy, Richard J., Smith, Alasdair R.C., Sundaram, Hardy, Vrolijk, David, Weston, Mark A., Wishart, Grant, Wren, Paul
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 01.02.2005 Elsevier
Subjects:	Analgesia Analgesics Animals Biological and medical sciences CHO Cells Cricetinae Cyclic AMP - biosynthesis Drug Design Humans Hydrophobic and Hydrophilic Interactions Inhibitory Concentration 50 Male Medical sciences Mice Neuropharmacology Nociception Opioid ORL1 Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - pharmacology Receptors, Opioid - agonists Structure-Activity Relationship Transfection Vas Deferens Nociception Opioid Analgesia ORL1 Agonist Intravenous administration Rodentia Selectivity In vitro In vivo Vertebrata Mammalia Analgesic Structure activity relation Mouse Benzimidazole derivatives N/OFQ receptor Animal Piperidine derivatives Chemical synthesis
ISSN:	0960-894X, 1464-3405
Online Access:	Get full text
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