| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10594774 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
A series of 5-HT6 ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several neutral, 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-HT6 for antagonism.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ralph N. III, Russel S. Stabler, David B. Repke, James M. Kress, Keith A. Walker, Renee S. Martin, Julie M. Brothers, Mariola Ilnicka, Simon W. Lee, Tara Mirzadegan,