Abstract
To further extend the structure-activity relationships of levorphanol, two series of novel morphinans were prepared by incorporation of an indole or aminothiazole fragment to the hexyl ring (ring C) in levorphanol. Such morphinans differed from previously reported ligands in that such indole- or aminothiazole-containing morphinans displayed enhanced binding affinity to the delta opioid receptor, while the affinity to kappa and micro receptors was slightly reduced.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Analgesics, Opioid / chemical synthesis*
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Analgesics, Opioid / pharmacology
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Animals
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CHO Cells
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Cricetinae
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Cricetulus
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Levorphanol / analogs & derivatives*
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Levorphanol / chemical synthesis*
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Levorphanol / pharmacology
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Radioligand Assay
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Structure-Activity Relationship
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Thiazoles / chemical synthesis*
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Thiazoles / pharmacology
Substances
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Analgesics, Opioid
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Indoles
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Thiazoles
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Levorphanol