Abstract
Twenty-four 3-alkyl-(5,5'-diphenyl)imidazolidinediones were synthesized and evaluated as new cannabinoid receptor ligands. Three compounds exhibited a Ki value around 100 nM against [3H]-SR 141716A binding obtained from human CB1 transfected CHO cells membranes. The lack of change of affinity in the presence of a non hydrolyzable GTP analogue seems to indicate they are cannabinoid antagonists.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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CHO Cells
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Cannabinoids*
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Cricetinae
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology
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Ligands
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Piperidines / pharmacology
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Pyrazoles / pharmacology
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Receptors, Cannabinoid
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Receptors, Drug / antagonists & inhibitors*
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Rimonabant
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Structure-Activity Relationship
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Transfection
Substances
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Cannabinoids
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Imidazoles
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Ligands
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Piperidines
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Pyrazoles
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Receptors, Cannabinoid
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Receptors, Drug
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Rimonabant