Title of article
Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone
Author/Authors
Mark P. Wentland، نويسنده , , Qun Lu، نويسنده , , Rongliang Lou، نويسنده , , Yigong Bu، نويسنده , , Brian I. Knapp، نويسنده , , Jean M. Bidlack، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
2107
To page
2110
Abstract
Very high affinity for opioid receptors (e.g., Ki = 0.052 nM for μ) 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.
Keywords
Opiate , SAR
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795541
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