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Medicine and Health Sciences

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University of Mississippi

Theses/Dissertations

2012

G-protien-coupled receptors

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Design Synthesis And Biological Evaluation Of Non-Peptide Neuropeptide Ff Ligands, Jessica Valentinas Mankus Jan 2012

Design Synthesis And Biological Evaluation Of Non-Peptide Neuropeptide Ff Ligands, Jessica Valentinas Mankus

Electronic Theses and Dissertations

Neuropeptide FF is an endogenous RF-amide with two receptor subtypes originally described as having anti-opioid characteristics. While peptide work helped to elucidate key features for targeting the subtypes of the neuropeptide FF receptor, non-peptide small molecules offer a more refined tool to discover features that affect selectivity and affinity. Improvements in small molecule ligands for neuropeptide FF support lead development and offer a clearer understanding of the binding pocket of each receptor subtype. Previous work on the lead 4–anilindopiperidine structure clarified a key feature between agonist and antagonist behavior. Early modifications of substituents of the piperidine nitrogen were tolerated and …