Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor

R B Westkaemper; S P Runyon; J E Savage; B L Roth; R A Glennon

doi:10.1016/s0960-894x(01)00010-5

Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor

Bioorg Med Chem Lett. 2001 Feb 26;11(4):563-6. doi: 10.1016/s0960-894x(01)00010-5.

Authors

R B Westkaemper¹, S P Runyon, J E Savage, B L Roth, R A Glennon

Affiliation

¹ Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298, USA. richard.westkaemper@vcu.edu

PMID: 11229772
DOI: 10.1016/s0960-894x(01)00010-5

Abstract

Comparison of the serotonin 5-HT2A receptor affinities of a parallel series of structural analogues of the novel ligand 9-aminomethyl-9,10-dihydroanthracene (AMDA) and a structurally similar prototypical tricyclic amine cyproheptadine suggests that the two agents bind to the receptor in different fashions. Examination of ligand-receptor model complexes supports the experimental data and suggests a potential origin for the differences in binding modes.

Publication types

Research Support, U.S. Gov't, P.H.S.

MeSH terms

3T3 Cells
Animals
Anthracenes / metabolism*
Cyproheptadine / metabolism*
Mice
Models, Molecular
Molecular Conformation
Receptor, Serotonin, 5-HT2A
Receptors, Serotonin / metabolism*
Serotonin Antagonists / metabolism*
Structure-Activity Relationship

Substances

9-(aminomethyl)-9,10-dihydroanthracene
Anthracenes
Receptor, Serotonin, 5-HT2A
Receptors, Serotonin
Serotonin Antagonists
Cyproheptadine

Grants and funding

etc