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Start Over Author "Ilnicka M" Journal bioorganic medicinal chemistry letters

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1. Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism.

Author

Harris RN 3rd, Stabler RS, Repke DB, Kress JM, Walker KA, Martin RS, Brothers JM, Ilnicka M, Lee SW, and Mirzadegan T

Subjects
Ligands, Models, Molecular, Mutagenesis, Site-Directed, Structure-Activity Relationship, Receptors, Serotonin metabolism
Abstract

A series of 5-HT(6) ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new alternative binding mode to 5-HT(6) for antagonism., (Copyright 2010. Published by Elsevier Ltd.)

Published
2010
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