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Updated: Sep 25, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Bivalent biogenic amine reuptake inhibitors
Keith Fandrick1, Xianqi Feng, Aaron Janowsky
1Human BioMolecular Research Institute, 5310 Eastgate Mall, 92121, San Diego, CA, USA.
Abstract:
A series of aryltropane-based bivalent ligands was prepared and investigated for binding potency and for their ability to inhibit reuptake of human dopamine, serotonin and norepinephrine transporters. The bivalent ligand 4, comprised of linking an aryltropane by an octamethylene spacer showed high efficacy for the human dopamine transporter and had a discrimination ratio of 130.
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