Abstract
A novel series of indolin-2-ones having a spirocyclic piperidine ring at the 3-position was synthesized and found to bind with high affinity to the ORL-1 receptor. Structure-activity relationships at the piperidine nitrogen were investigated. Substitution on the phenyl ring and nitrogen atom of the indolin-2-one core generated several selective high-affinity ligands that were antagonists of the ORL-1 receptor.
MeSH terms
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Acetates / chemistry
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Cell Line
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Cyclization
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / metabolism*
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Indoles / pharmacology
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Inhibitory Concentration 50
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Ligands
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Molecular Structure
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Narcotic Antagonists
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Nociceptin Receptor
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Receptors, Opioid / metabolism*
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Structure-Activity Relationship
Substances
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Acetates
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Indoles
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Ligands
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Narcotic Antagonists
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Receptors, Opioid
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indolin-2-one
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Nociceptin Receptor
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OPRL1 protein, human