Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.

Article Details

Citation

Keith JM, Gomez LA, Letavic MA, Ly KS, Jablonowski JA, Seierstad M, Barbier AJ, Wilson SJ, Boggs JD, Fraser IC, Mazur C, Lovenberg TW, Carruthers NI

Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):702-6. Epub 2006 Nov 2.

PubMed ID
17107798 [ View in PubMed
]
Abstract

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
FluoxetineSodium-dependent serotonin transporterKi (nM)2N/AN/ADetails