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- W62964987 abstract "The kappa opioid receptor (KOR), a member of the opioid receptor family, was initially studied for its involvement in the mediation of pain. More recently, there has been growing interest in selective KOR agents for their potential effects on mood and reward. In particular, selective KOR antagonists may offer a novel approach to relieve symptoms of depression. In this chapter, we describe the structure–activity relationships (SAR) of nonpeptidic KOR antagonists. Specifically, we review the SAR of norbinaltorphimine (norBNI) and its structur ally simplified derivative GNTI. We present the SAR of JDTic and the recently developed MTHQ. The SAR patterns of norBNI have been extensively studied, but there have been relatively fewer studies on the SAR of JDTic and MTHQ. While the overall SAR trends of these structurally distinct agents differ, there appears to be a common requirement for KOR inhibition: the presence of a phenol unit and a basic nitrogen. In the second part of this chapter, we discuss the unusually long duration of action of the available KOR antagonists and make suggestions on pos sibilities for the design of additional KOR antagonists.Keywords:Kappa opioid receptorsStructure–activity relationshipNonpeptidic antagonistsnorBNIGNTIJDTicMTHQ" @default.
- W62964987 created "2016-06-24" @default.
- W62964987 creator A5085625764 @default.
- W62964987 creator A5091796070 @default.
- W62964987 date "2009-01-01" @default.
- W62964987 modified "2023-10-14" @default.
- W62964987 title "Medicinal Chemistry of Kappa Opioid Receptor Antagonists" @default.
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- W62964987 doi "https://doi.org/10.1007/978-1-59745-197-0_6" @default.
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