Author/Authors :
John M. Keith، نويسنده , , Leslie A. Gomez، نويسنده , , Ronald L. Wolin، نويسنده , , Ann J. Barbier، نويسنده , , Sandy J. Wilson، نويسنده , , Jamin D. Boggs، نويسنده , , Curt Mazur، نويسنده , , Ian C. Fraser، نويسنده , , Brian Lord، نويسنده , , Leah Aluisio، نويسنده , , Timothy W. Lovenberg، نويسنده , , Nicholas I. Carruthers، نويسنده ,
Abstract :
A series of novel and potent pyrrolidino-tetrahydroisoquinolines with dual histamine H3 antagonist/serotonin transporter inhibitor activity is described. A highly regio- and diastereoselective synthesis of the pyrrolidino-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.
Keywords :
Histamine H3 , Serotonin transporter , microdialysis , reduction
