Title

Serotonin transporter inhibitors: synthesis and binding potency of 2′-methyl- and 3′-methyl-6-nitroquipazine

Authors

John M. Gerdes, Central Washington University
Steven C. DeFina, Central Washington University
Paul A. Wilson, Central Washington University
Scott E. Taylor, Lawrence Berkeley National Laboratory

Document Type

Article

Department or Administrative Unit

Chemistry

Publication Date

12-4-2000

Abstract

Racemic 2′-methyl- and 3′-methyl-6-nitroquipazine ligands were selected as targets, synthesized and evaluated at the serotonin transporter employing an in vitro competitive inhibition assay with [³H]paroxetine and rat cortical membrane. The 2′-methyl-6-nitroquipazine was found to be 50 times more potent than the 3′-methyl-substituted counterpart and of comparable potency to the known high affinity agent 5-iodo-6-nitroquipazine.

Comments

This article was originally published in Bioorganic & Medicinal Chemistry Letters. The full-text article from the publisher can be found here.

Due to copyright restrictions, this article is not available for free download from ScholarWorks @ CWU.

Recommended Citation

Gerdes, J. M., DeFina, S. C., Wilson, P. A., & Taylor, S. E. (2000). Serotonin transporter inhibitors: synthesis and binding potency of 2′-methyl- and 3′-methyl-6-nitroquipazine. Bioorganic & Medicinal Chemistry Letters, 10(23), 2643–2646. https://doi.org/10.1016/s0960-894x(00)00546-1

Journal

Bioorganic & Medicinal Chemistry Letters

Rights

Copyright © 2000 Elsevier Science Ltd. All rights reserved.