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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. doi: 10.1016/j.bmcl.2010.01.101. Epub 2010 Jan 25.

Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.

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1
Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA. b.fulton@neu.edu

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.

PMID:
20144870
PMCID:
PMC2834170
DOI:
10.1016/j.bmcl.2010.01.101
[Indexed for MEDLINE]
Free PMC Article
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