Author/Authors :
John M. Keith، نويسنده , , Ann J. Barbier، نويسنده , , Sandy J. Wilson، نويسنده , , Kirstin Miller، نويسنده , , Jamin D. Boggs، نويسنده , , Ian C. Fraser، نويسنده , , Curt Mazur، نويسنده , , Timothy W. Lovenberg، نويسنده , , Nicholas I. Carruthers، نويسنده ,
Abstract :
A series of tetrahydroisoquinolines acting as dual serotonin transporter inhibitor/histamine H3 antagonists is described. The introduction of polar aromatic spacers as part of the histamine H3 pharmacophore was explored. A convergent synthesis of the final products allowing late stage introduction of the aromatic side chain was developed. In vitro and in vivo data are discussed.
Keywords :
tetrahydroisoquinoline , SERT , Histamine H3 , Serotonin
