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Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.
Bioorganic & Medicinal Chemistry Letters 2007 Februrary 2
A series of tetrahydroisoquinolines acting as dual histamine H3/serotonin transporter ligands is described. A highly regio-selective synthesis of the tetrahydroisoquinoline core involving acid mediated ring-closure of an acetophenone intermediate followed by reduction with NaCNBH3 was developed. In vitro and in vivo data are discussed.
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