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

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.

Journal

Bioorganic & Medicinal Chemistry Letters

Rights

Copyright © 2000 Elsevier Science Ltd. All rights reserved.

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