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

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Wentland MP, Lu Q, Lou R, Bu Y, Knapp BI, Bidlack JM

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

Bioorg Med Chem Lett. 2005 Apr 15;15(8):2107-10. doi: 10.1016/j.bmcl.2005.02.032.

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15808478 [ View in PubMed
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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.

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