Abstract
A series of 7,8- and 8,9-fused triazole and imidazole analogues of cyclazocine have been made and characterized in opioid receptor binding and [(35)S]GTPgammaS assays. Target compounds were designed to explore the SAR surrounding our lead molecule for this study, namely the 8,9-fused pyrrolo analogue 2 of cyclazocine. Compared to 2, many of the new compounds in this study displayed very high affinity for opioid receptors.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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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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Cyclazocine / analogs & derivatives
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Cyclazocine / chemical synthesis*
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Cyclazocine / metabolism
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Cyclazocine / pharmacology*
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Cyclization
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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Radioligand Assay
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Receptors, Opioid / drug effects*
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Receptors, Opioid / metabolism
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Structure-Activity Relationship
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Sulfur Radioisotopes
Substances
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Receptors, Opioid
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Sulfur Radioisotopes
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Guanosine 5'-O-(3-Thiotriphosphate)
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Cyclazocine