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