Abstract
A series of aminoalkylazetidines has been discovered as novel ORL1 receptor ligands. Structure-activity relationships have been investigated at the azetidine N and the alkyl side chain sites. Several potent and selective analogues have been identified.
MeSH terms
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Animals
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Azetidines / chemical synthesis*
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Azetidines / pharmacology*
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Binding, Competitive / drug effects
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CHO Cells
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Cricetinae
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Diprenorphine / pharmacology
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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Humans
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Indicators and Reagents
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Ligands
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Narcotic Antagonists / pharmacology
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Nociceptin
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Nociceptin Receptor
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Opioid Peptides / metabolism
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Receptors, Opioid / drug effects*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Azetidines
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Indicators and Reagents
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Ligands
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Narcotic Antagonists
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Opioid Peptides
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Receptors, Opioid
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Diprenorphine
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Guanosine 5'-O-(3-Thiotriphosphate)
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Nociceptin Receptor