Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.
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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
Drug Target Property Measurement pH Temperature (°C) Fluoxetine Sodium-dependent serotonin transporter Ki (nM) 2 N/A N/A Details