Abstract
A series of bivalent hydroxy ether butorphan ligands were prepared and their binding affinities at the opioid receptors determined. Addition of a hydroxy group to a hydrocarbon chain can potentiate binding affinity up to 27- and 86-fold at the mu and kappa opioid receptors, respectively. Two bivalent ligands with sub-nanomolar binding affinity at the mu and kappa opioid receptors were discovered.
Copyright 2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Analgesics / chemical synthesis
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Analgesics / chemistry*
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Analgesics / 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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Ligands*
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Morphinans / chemical synthesis
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Morphinans / chemistry*
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Morphinans / pharmacology
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Protein Binding
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Receptors, Opioid, kappa / antagonists & inhibitors
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Receptors, Opioid, kappa / metabolism*
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Receptors, Opioid, mu / antagonists & inhibitors
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Receptors, Opioid, mu / metabolism*
Substances
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Analgesics
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Ligands
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Morphinans
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Receptors, Opioid, kappa
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Receptors, Opioid, mu
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butorphan