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Bioorg Med Chem Lett. 2005 Apr 15;15(8):2107-10.

Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.

Author information

1
Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, NY 12180, USA. wentmp@rpi.edu <wentmp@rpi.edu>

Abstract

Very high affinity for opioid receptors (e.g., K(i)=0.052nM for mu) has been observed in the rationally designed naltrexone analogue 5. SAR and physical data supports the hypothesis that the 4-OH group of 5 stabilizes the 3-carboxamido group in the putative bioactive conformation.

PMID:
15808478
DOI:
10.1016/j.bmcl.2005.02.032
[Indexed for MEDLINE]

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