1235513-75-3Relevant academic research and scientific papers
Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism
Harris III, Ralph N.,Stabler, Russel S.,Repke, David B.,Kress, James M.,Walker, Keith A.,Martin, Renee S.,Brothers, Julie M.,Ilnicka, Mariola,Lee, Simon W.,Mirzadegan, Tara
scheme or table, p. 3436 - 3440 (2010/07/16)
A series of 5-HT6 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-HT6 for antagonism.
