Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors

Manik R Pullagurla; Richard B Westkaemper; Richard A Glennon

doi:10.1016/j.bmcl.2004.05.076

Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4569-73. doi: 10.1016/j.bmcl.2004.05.076.

Authors

Manik R Pullagurla¹, Richard B Westkaemper, Richard A Glennon

Affiliation

¹ Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298-0540, USA.

PMID: 15357994
DOI: 10.1016/j.bmcl.2004.05.076

Abstract

A graphics model of the human 5-HT6 receptor was constructed and automated docking studies were performed. The model suggests that 5-HT6 antagonist arylsulfonyltryptamines might bind differently than that of the agonist serotonin. Furthermore, the model explains many of the empirical results from our previous structure-affinity studies.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

MeSH terms

Humans
Protein Binding / physiology
Receptors, Serotonin / metabolism*
Serotonin Antagonists / chemistry*
Serotonin Antagonists / metabolism*
Serotonin Receptor Agonists / chemistry*
Serotonin Receptor Agonists / metabolism*

Substances

Receptors, Serotonin
Serotonin Antagonists
Serotonin Receptor Agonists
serotonin 6 receptor

Grants and funding

MH60599/MH/NIMH NIH HHS/United States