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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

10.1016/j.bmcl.2010.03.110

subject

Has Abstract

pub_date

2010-06-01 00:00:00

pages

3436-40

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00451-8

journal_volume

20

pub_type

杂志文章

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