Abstract
A series of furanomorphides were synthesised as ring-constrained analogues of buprenorphine and related orvinols. Evaluation in binding and functional assays has shown that the furanomorphides have reduced efficacy at the mu opioid receptor compared to the orvinols.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Brain / drug effects
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Buprenorphine / analogs & derivatives*
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Buprenorphine / pharmacology
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CHO Cells
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Cricetinae
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Furans / chemical synthesis*
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Guinea Pigs
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Inhibitory Concentration 50
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Kinetics
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Male
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Mice
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Models, Chemical
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Morphinans / chemical synthesis*
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Receptors, Opioid / drug effects
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Vas Deferens / drug effects
Substances
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Furans
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Morphinans
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Receptors, Opioid
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Buprenorphine